lavender

Generic Name: lavender (LAH ven der)

Brand Names:

What is lavender?

The use of lavender in cultural and traditional settings may differ from concepts accepted by current Western medicine. When considering the use of herbal supplements, consultation with a primary health care professional is advisable. Additionally, consultation with a practitioner trained in the uses of herbal/health supplements may be beneficial, and coordination of treatment among all health care providers involved may be advantageous.

Lavender is also known as Lavandula angustifolia, aspic, lavandin, spike lavender, and true lavender.

Lavender has been used for many purposes including loss of appetite, nervousness, insomnia, acne, headaches, diabetes, rheumatic pain, nerve pain, and colds.

Lavender has not been evaluated by the FDA for safety, effectiveness, or purity. All potential risks and/or advantages of lavender may not be known. Additionally, there are no regulated manufacturing standards in place for these compounds. There have been instances where herbal/health supplements have been sold which were contaminated with toxic metals or other drugs. Herbal/health supplements should be purchased from a reliable source to minimize the risk of contamination.

Lavender may also have uses other than those listed in this product guide.

What is the most important information I should know about lavender?

Use caution when driving, operating machinery, or performing other hazardous activities. At higher doses, lavender may cause drowsiness. If you experience drowsiness, avoid these activities. Avoid alcohol while taking lavender. Alcohol may increase drowsiness caused by lavender.

At higher doses, lavender may increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, antihistamines, sedatives (used to treat insomnia), pain relievers, anxiety medicines, seizure medicines, and muscle relaxants. Do not take lavender with other medications that may also cause drowsiness.

Lavender has not been evaluated by the FDA for safety, effectiveness, or purity. All potential risks and/or advantages of lavender may not be known. Additionally, there are no regulated manufacturing standards in place for these compounds. There have been instances where herbal/health supplements have been sold which were contaminated with toxic metals or other drugs. Herbal/health supplements should be purchased from a reliable source to minimize the risk of contamination.

What should I discuss with my health care provider before using lavender?

Before taking lavender, talk to your doctor, pharmacist, or health care professional if you have allergies (especially to plants), have any medical condition, or if you take other medicines or other herbal/health supplements. Lavender may not be recommended in some situations.

Do not take lavender without first talking to your doctor if you are pregnant or could become pregnant. It is not known whether lavender will harm an unborn baby. Do not take lavender without first talking to your doctor if you are breast-feeding a baby. It is also not known whether lavender will harm a nursing infant. There is no information available regarding the use of lavender by children. Do not give any herbal/health supplement to a child without first talking to the child's doctor.

How should I take lavender?

The use of lavender in cultural and traditional settings may differ from concepts accepted by current Western medicine. When considering the use of herbal supplements, consultation with a primary health care professional is advisable. Additionally, consultation with a practitioner trained in the uses of herbal/health supplements may be beneficial, and coordination of treatment among all health care providers involved may be advantageous.

If you choose to take lavender, use it as directed on the package or as directed by your doctor, pharmacist, or other health care provider.

Standardized extracts, tinctures, and solid formulations of herbal/health supplements may provide a more reliable dose of the product.

Take the pill forms of lavender with a full glass of water.

To ensure the correct dose, measure the liquid forms of lavender with a dropper or a dose-measuring spoon or cup.

Some forms of lavender can be brewed to form a tea for drinking.

Do not use different formulations (e.g., liquids, teas, and others) of lavender at the same time, unless specifically directed to do so by a health care professional. Using different formulations together increases the risk of an overdose of lavender.

Store lavender as directed on the package. In general, lavender should be protected from light.

What happens if I miss a dose?

Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra lavender to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking lavender?

Use caution when driving, operating machinery, or performing other hazardous activities. At higher doses, lavender may cause drowsiness. If you experience drowsiness, avoid these activities. Avoid alcohol while taking lavender. Alcohol may increase drowsiness caused by lavender.

At higher doses, lavender may increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, antihistamines, sedatives (used to treat insomnia), pain relievers, anxiety medicines, seizure medicines, and muscle relaxants. Do not take lavender with other medications that may also cause drowsiness.

Lavender side effects

Although rare, allergic reactions to lavender may occur. Stop taking lavender and seek emergency medical attention if you experience symptoms of a serious allergic reaction including difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect lavender?

Avoid alcohol while taking lavender. Alcohol may increase drowsiness caused by lavender.

At higher doses, lavender may increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, antihistamines, sedatives (used to treat insomnia), pain relievers, anxiety medicines, seizure medicines, and muscle relaxants. Do not take lavender with other medications that may also cause drowsiness.

Interactions between lavender and other prescription or over-the-counter medicines or herbal/health supplements may also occur. Talk to your doctor, pharmacist, or health care professional before taking lavender if you are taking any other medicines or supplements.

More lavender resources

• Lavender Support Group
• 0 Reviews for Lavender - Add your own review/rating

• Lavender Natural MedFacts for Professionals (Wolters Kluwer)


• Lavender Natural MedFacts for Consumers (Wolters Kluwer)

Compare lavender with other medications

• Acne
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Where can I get more information?

• Consult with a licensed healthcare professional before using any herbal/health supplement. Whether you are treated by a medical doctor or a practitioner trained in the use of natural medicines/supplements, make sure all your healthcare providers know about all of your medical conditions and treatments.

Latuda

Generic Name: Lurasidone Hydrochloride
Class: Atypical Antipsychotics
VA Class: CN709
Chemical Name: monohydrochloride (3aR,4S,7R,7aS)-4,3(2H)-dione, 2 - [[(1R,2R) - 2 - [[4 - (1,2 - benzisothiazol - 3 - yl) - 1 - piperazinyl]methyl]cyclohexyl]methyl]hexahydro - ,7 - Methano - 1H - isoindole - 1
Molecular Formula: C₂₈H₃₆N₄O₂S•HCl
CAS Number: 367514-88-3

• Increased Mortality in Geriatric Patients with Dementia-related Psychosis


• 
  

  Geriatric patients with dementia-related psychosis treated with antipsychotic agents are at an increased risk of death.^{1 28 39 73 75}

  
  


• 
  

  Analyses of 17 placebo-controlled trials in geriatric patients mainly receiving atypical antipsychotic agents revealed an approximate 1.6- to 1.7-fold increase in mortality compared with that in patients receiving placebo.^{1 39 73}

  
  


• 
  

  Most fatalities appeared to result from cardiovascular-related events (e.g., heart failure, sudden death) or infections (mostly pneumonia).^{1 73}

  
  


• 
  

  Observational studies suggest that conventional or first-generation antipsychotic agents also may increase mortality in such patients.^{1 28 39}

  
  


• 
  

  Antipsychotic agents, including lurasidone, are not approved for the treatment of dementia-related psychosis.^{1 39 73}

  
  

Introduction

benzisothiazol-derivative; atypical or second-generation antipsychotic agent.^{1 2 8 9}

Uses for Latuda

Schizophrenia

Acute treatment of schizophrenia in adults.^{1 2 4 5 8}

American Psychiatric Association (APA) considers most atypical antipsychotic agents first-line drugs for management of the acute phase of schizophrenia (including first psychotic episodes).²⁸

Patients who do not respond to or tolerate one drug may be successfully treated with an agent from a different class or with a different adverse effect profile.^{28 70 71 72}

Latuda Dosage and Administration

Administration

Oral Administration

Administer tablets orally once daily, usually in the morning or evening.^{1 9} Take with food (containing at least 350 calories).¹ (See Food under Pharmacokinetics.)

Dosage

Available as lurasidone hydrochloride; dosage expressed in terms of the hydrochloride salt.¹

If used with a moderate CYP3A4 inhibitor, dosage adjustment may be required.¹ (See Contraindications under Cautions and also see Interactions.)

Adults

Schizophrenia

Oral

For acute treatment, recommended initial dosage is 40 mg once daily.¹ Initial dosage titration not required.^{1 9} Although dosages ranging from 40–120 mg daily were effective in controlled trials,¹ the highest dosage (120 mg daily) did not provide additional therapeutic benefit but was associated with a dose-related increase in certain adverse effects.¹ Maximum recommended dosage is 80 mg daily.¹

Long-term (i.e., >6 weeks) efficacy of lurasidone not systematically evaluated in controlled trials.¹ In responsive patients, continue drug therapy beyond the acute response and as long as clinically necessary and tolerated; periodically reassess need for continued therapy.^{1 28}

In patients with remitted first or multiple episodes, APA recommends either indefinite maintenance therapy or gradual discontinuance of the antipsychotic with close follow-up and a plan to reinstitute treatment upon symptom recurrence.²⁸ Consider antipsychotic therapy discontinuance only after ≥1 year of symptom remission or optimal response while receiving the drug.²⁸ Indefinite maintenance treatment recommended if patient has experienced multiple previous psychotic episodes or 2 episodes within 5 years.²⁸

Prescribing Limits

Adults

Schizophrenia

Oral

Maximum 80 mg daily.¹

Special Populations

Hepatic Impairment

Moderate (Child-Pugh class B) or severe (Child-Pugh class C) hepatic impairment: Do not exceed 40 mg daily.¹

Mild hepatic impairment (Child-Pugh class A): Dosage adjustment does not appear necessary.¹ (See Hepatic Impairment under Cautions.)

Renal Impairment

Moderate or severe renal impairment: Do not exceed 40 mg daily.¹

Mild renal impairment: Dosage adjustment does not appear necessary.¹ (See Renal Impairment under Cautions.)

Geriatric Patients

Dosage adjustment not required.¹

Gender or Race

Dosage adjustment not recommended based on gender or race.¹

Cautions for Latuda

Contraindications

• 
  

  Known hypersensitivity to lurasidone hydrochloride or any components in the formulation.¹ Angioedema reported.¹

  
  


• 
  

  Concurrent administration of strong CYP3A4 inhibitors (e.g., ketoconazole) or strong CYP3A4 inducers (e.g., rifampin).¹ (See Interactions.)

  
  

Warnings/Precautions

Warnings

Increased Mortality in Geriatric Patients with Dementia-related Psychosis

Increased risk of death with use of either conventional (first-generation) or atypical (second-generation) antipsychotics in geriatric patients with dementia-related psychosis.^{1 28 39 73 75}

Antipsychotic agents, including lurasidone, are not approved for the treatment of dementia-related psychosis.^{1 39 73} (See Increased Mortality in Geriatric Patients with Dementia-related Psychosis in Boxed Warning, see Cerebrovascular Events in Geriatric Patients with Dementia-related Psychosis under Cautions, and see Dysphagia under Cautions.)

Sensitivity Reactions

Rash and pruritus reported frequently; angioedema reported rarely.¹ (See Contraindications under Cautions.)

Other Warnings and Precautions

Cerebrovascular Events in Geriatric Patients with Dementia-related Psychosis

Increased incidence of adverse cerebrovascular events (cerebrovascular accidents and TIAs), including fatalities, observed in geriatric patients with dementia-related psychosis treated with certain atypical antipsychotic agents (aripiprazole, olanzapine, risperidone) in placebo-controlled studies.^{1 28} Lurasidone is not approved for the treatment of dementia-related psychosis.¹ (See Increased Mortality in Geriatric Patients with Dementia-related Psychosis in Boxed Warning.)

Neuroleptic Malignant Syndrome

Neuroleptic malignant syndrome (NMS), a potentially fatal syndrome characterized by hyperpyrexia, muscle rigidity, altered mental status, and autonomic instability, reported with antipsychotic agents, including lurasidone.¹

Immediately discontinue therapy and initiate supportive and symptomatic treatment if NMS occurs.¹ Careful monitoring recommended if therapy is reinstituted following recovery; the risk that NMS can recur must be considered.¹

Tardive Dyskinesia

Tardive dyskinesia, a syndrome of potentially irreversible, involuntary dyskinetic movements, reported with use of antipsychotic agents, including lurasidone.¹

Reserve long-term antipsychotic treatment for patients with chronic illness known to respond to antipsychotic agents, and for whom alternative, equally effective, but potentially less harmful treatments are not available or appropriate.¹ In patients requiring chronic treatment, use smallest dosage and shortest duration of treatment producing a satisfactory clinical response; periodically reassess need for continued therapy.¹

APA recommends assessing patients receiving atypical antipsychotic agents for abnormal involuntary movements every 12 months; for patients at increased risk for tardive dyskinesia, assess every 6 months.²⁸ Consider discontinuance of lurasidone if signs and symptoms of tardive dyskinesia appear.¹ However, some patients may require treatment despite presence of the syndrome.¹

Metabolic Changes

Atypical antipsychotic agents are associated with metabolic changes that may increase cardiovascular and cerebrovascular risk (e.g., hyperglycemia, dyslipidemia, weight gain).¹ While all atypical antipsychotics produce some metabolic changes, each drug has its own specific risk profile.¹ (See Hyperglycemia and Diabetes Mellitus, see Dyslipidemia, and also see Weight Gain under Cautions.)

Hyperglycemia and Diabetes Mellitus

Hyperglycemia, sometimes severe and associated with ketoacidosis, hyperosmolar coma, or death, reported in patients receiving atypical antipsychotic agents.^{1 11 12 14 15 16 17 18 20 21 22 23 25 31 40 41 42 46 65} In short-term clinical trials, clinically important differences between lurasidone and placebo in mean change from baseline to end point in serum glucose concentrations not observed.¹

Closely monitor patients with an established diagnosis of diabetes mellitus for worsening of glucose control and perform fasting blood glucose testing at baseline and periodically in patients with risk factors for diabetes (e.g., obesity, family history of diabetes).^{1 11 12 14 15 16 17 18 19 20 21 22 23 31 83} If manifestations of hyperglycemia occur in any lurasidone-treated patient, perform fasting blood glucose testing.^{1 11 12 14 15 16 17 18 19 20 21 22 23 31 83} (See Advice to Patients.)

Some patients who developed hyperglycemia while receiving an atypical antipsychotic have required continuance of antidiabetic treatment despite discontinuance of the suspect drug; in other patients, hyperglycemia resolved with discontinuance of the antipsychotic.^{1 11 12 14 15 16 17 18 19 20 21 22 23 31 46 83}

Dyslipidemia

Undesirable changes in lipid parameters observed in patients treated with some atypical antipsychotics.^{1 9} In clinical studies, clinically important effects of lurasidone on serum lipids not observed.¹

Weight Gain

Weight gain observed with atypical antipsychotic therapy.^{1 9} Although lurasidone generally produces minimal weight gain compared with some other atypical antipsychotic agents (e.g., olanzapine),^{1 2 9 82} manufacturer recommends clinical monitoring of weight during lurasidone therapy.¹ (See Hyperglycemia and Diabetes Mellitus under Cautions)

Hyperprolactinemia

May cause elevated serum prolactin concentrations, which may persist during chronic administration and cause clinical disturbances (e.g., galactorrhea, amenorrhea, gynecomastia, impotence); chronic hyperprolactinemia associated with hypogonadism may lead to decreased bone density in both females and males.^{1 2 4}

If contemplating lurasidone therapy in a patient with previously detected breast cancer, consider that approximately one-third of human breast cancers are prolactin-dependent in vitro.¹

Hematologic Effects

Leukopenia and neutropenia temporally related to antipsychotic agents, including lurasidone, reported during clinical trial and/or postmarketing experience.^{1 31 78} Agranulocytosis (including fatal cases) also reported with other antipsychotic agents.¹

Possible risk factors for leukopenia and neutropenia include preexisting low WBC count and a history of drug-induced leukopenia or neutropenia.^{1 78} Monitor CBC frequently during the first few months of therapy in patients with such risk factors.¹ Discontinue lurasidone at the first sign of a decline in WBC count in the absence of other causative factors.¹

Carefully monitor patients with neutropenia for signs and symptoms of infection (e.g., fever) and treat promptly if they occur.¹ Discontinue lurasidone if severe neutropenia (ANC <1000/mm³) occurs; monitor WBC until recovery occurs.¹

Orthostatic Hypotension and Syncope

Risk of orthostatic hypotension associated with dizziness, tachycardia or bradycardia, and syncope, particularly early in treatment, because of lurasidone's α₁-adrenergic blocking activity.¹ In short-term, placebo-controlled clinical trials, orthostatic hypotension and syncope reported in 0.4 and <0.1% of lurasidone-treated patients, respectively.¹

Use with caution in patients with known cardiovascular disease (e.g., heart failure, history of MI or ischemic heart disease, conduction abnormalities), cerebrovascular disease, or conditions that would predispose patients to develop hypotension (e.g., dehydration, hypovolemia, concomitant antihypertensive therapy) and in antipsychotic-naive patients.¹ Consider monitoring orthostatic vital signs in patients who are susceptible to hypotension.¹

Seizures

Seizures reported in <0.1% of lurasidone-treated patients compared with 0.2% of placebo recipients in short-term clinical trials.¹ Use with caution in patients with a history of seizures or with conditions that lower the seizure threshold (e.g., dementia of the Alzheimer’s type); conditions that lower seizure threshold may be more prevalent in patients ≥65 years of age.¹

Cognitive and Motor Impairment

Judgment, thinking, or motor skills may be impaired.¹ Somnolence (including hypersomnia, hypersomnolence, and sedation) reported in about 22% of lurasidone-treated patients in clinical trials; frequency of somnolence is dose-related.¹ (See Advice to Patients.)

Body Temperature Regulation

Antipsychotic agents may disrupt ability to regulate core body temperature.¹

Use appropriate caution in patients who will be experiencing conditions that may contribute to an elevation in core body temperature (e.g., strenuous exercise, extreme heat, concomitant use of agents with anticholinergic activity, dehydration).¹

Suicide

Attendant risk with psychotic illnesses; closely supervise high-risk patients.¹ Prescribe in the smallest quantity consistent with good patient management to reduce risk of overdosage.¹

Dysphagia

Esophageal dysmotility and aspiration associated with the use of antipsychotic agents.¹

Aspiration pneumonia is a common cause of morbidity and mortality in geriatric patients, particularly in those with advanced Alzheimer's dementia.¹ Lurasidone is not approved for the treatment of patients with dementia-related psychosis and should not be used in patients at risk for aspiration pneumonia.¹ (See Increased Mortality in Geriatric Patients with Dementia-related Psychosis in Boxed Warning.)

Concomitant Illnesses

Limited experience with lurasidone in patients with certain concomitant diseases.¹

Not adequately evaluated in patients with a recent history of MI or unstable cardiovascular disease.¹ (See Orthostatic Hypotension and Syncope under Cautions.)

Specific Populations

Pregnancy

Category B.¹

Risk for extrapyramidal and/or withdrawal symptoms (e.g., agitation, hypertonia, hypotonia, tardive dyskinetic-like symptoms, tremor, somnolence, respiratory distress, feeding disorder) in neonates exposed to antipsychotic agents during the third trimester; monitor neonates exhibiting such symptoms.^{1 79 80 81} Symptoms were self-limiting in some neonates but varied in severity; some infants required intensive support and prolonged hospitalization.^{1 79 80 81}

Lactation

Lurasidone distributes into milk in rats; not known whether lurasidone and/or its metabolites distribute into human milk.¹ Manufacturer generally recommends avoiding breast-feeding; consider only if potential benefit justifies potential risk to child.¹

Pediatric Use

Safety and effectiveness not established in pediatric patients.¹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.¹ (See Geriatric Patients under Dosage and Administration and also see Special Populations under Pharmacokinetics.)

Geriatric patients with dementia-related psychosis treated with either conventional or atypical antipsychotic agents are at an increased risk of death;^{1 39 73 75} increased incidence of cerebrovascular events also observed with certain atypical antipsychotic agents.¹ Lurasidone is not approved for the treatment of dementia-related psychosis.¹ (See Increased Mortality in Geriatric Patients with Dementia-related Psychosis in Boxed Warning and also see Cerebrovascular Events in Geriatric Patients with Dementia-related Psychosis under Cautions and Dysphagia under Cautions.)

Hepatic Impairment

Dosage adjustment recommended in patients with moderate or severe hepatic impairment (Child-Pugh class B or C).¹ (See Hepatic Impairment under Dosage and Administration and also see Special Populations under Pharmacokinetics.)

Renal Impairment

Dosage adjustment recommended in patients with moderate or severe renal impairment (Cl_cr 10 to less than 50 mL/minute).¹ (See Renal Impairment under Dosage and Administration and also see Special Populations under Pharmacokinetics.)

Common Adverse Effects

Somnolence (including hypersomnia, hypersomnolence, and sedation),^{1 2 4} akathisia,^{1 2 4} nausea,^{1 2 4} parkinsonism,¹ agitation.¹

Interactions for Latuda

Metabolized principally by CYP3A4.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction with moderate or strong CYP3A4 inhibitors and strong CYP3A4 inducers.¹ Avoid concurrent use of strong CYP3A4 inhibitors or strong CYP3A4 inducers.¹ Do not exceed lurasidone dosage of 40 mg daily if used concomitantly with moderate CYP3A4 inhibitors.¹ (See Specific Drugs under Interactions.)

Lurasidone is not a substrate of CYP isoenzymes 1A1, 1A2, 2A6, 4A11, 2B6, 2C8, 2C9, 2C19, 2D6, or 2E1; clinically important pharmacokinetic interactions with lurasidone and drugs that are inhibitors or inducers of these enzymes unlikely.¹

Specific Drugs

Drug	Interaction	Comments
Alcohol	Possible additive CNS effects1	Avoid concomitant use1
Anticholinergic agents	Possible disruption of body temperature regulation1	Use with caution1
CNS agents	Possible additive CNS effects1	Use with caution1
Digoxin	Increased peak plasma concentrations and AUCs of digoxin by about 9 and 13%, respectively1	Digoxin dosage adjustment not required1
Diltiazem	Increased peak serum concentrations and AUCs of lurasidone by about twofold1	Do not exceed a lurasidone dosage of 40 mg daily1
Hypotensive agents	Possible additive hypotensive effects; may result in orthostatic hypotension and syncope1	Use concomitantly with caution; consider monitoring orthostatic vital signs1
Ketoconazole	Increased peak serum concentrations and AUCs of lurasidone by 6.9 and 9 times, respectively1	Concomitant use contraindicated1
Lithium	Decreased lurasidone peak serum concentrations by 10% and increased lurasidone AUCs by 1.1 times1	Lurasidone dosage adjustment not required1
Midazolam	Increased peak plasma concentrations and AUCs of midazolam by approximately 21 and 44%, respectively1	Midazolam dosage adjustment not required1
Oral contraceptives	Peak plasma concentrations and AUCs of oral contraceptives not substantially affected Sex hormone binding globulin concentrations not substantially affected1	Oral contraceptive dosage adjustment is not required1
Rifampin	Decreased peak serum concentrations and AUCs of lurasidone by approximately 86 and 80%, respectively1	Concomitant use contraindicated1
Smoking	Lurasidone is not a substrate for CYP1A2 in vitro; smoking unlikely to alter lurasidone pharmacokinetics1

Latuda Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed following oral administration; peak serum concentrations achieved within about 1–3 hours.^{1 9}

Approximately 9–19% of an orally administered dose is absorbed.¹

Steady-state concentrations of lurasidone achieved within 7 days.¹

Food

Mean peak serum concentrations and AUCs of lurasidone increased by about threefold and twofold, respectively, when administered with food compared with values obtained under fasting conditions.¹ Exposure not affected as meal size increased from 350 to 1000 calories and was independent of fat content.¹

Special Populations

In patients with mild, moderate, and severe renal impairment, mean peak serum concentrations of lurasidone increased by 40, 92, and 54%, respectively, and mean AUCs increased by 53%, 91%, and twofold, respectively, compared with healthy individuals.¹

Mean AUCs were 1.5, 1.7, and 3 times higher in individuals with mild (Child-Pugh class A), moderate (Child-Pugh class B), and severe hepatic impairment (Child-Pugh class C), respectively, compared with healthy individuals.¹ Mean peak serum concentrations were 1.3, 1.2, and 1.3 times higher for patients with mild, moderate, and severe hepatic impairment, respectively, compared with healthy individuals.¹

In geriatric patients with psychosis, serum lurasidone concentrations were similar to those observed in younger adults.¹

Distribution

Extent

Lurasidone distributes into milk in rats; not known whether the drug and/or its metabolites distribute into human milk.¹

Plasma Protein Binding

Highly bound (99.8%), including to albumin and α₁-acid glycoprotein.^{1 9}

Elimination

Metabolism

Metabolized mainly via CYP3A4.¹ Major biotransformation pathways are oxidative N-dealkylation, hydroxylation of norbornane ring, and S-oxidation.¹

Metabolized into 2 active metabolites (ID-14283 and ID-14326) and 2 major inactive metabolites (ID-20219 and ID-20220); pharmacologic activity primarily due to parent drug.¹

Elimination Route

Following administration of a single radiolabeled dose, about 89% of the dose was recovered; approximately 80% recovered in feces and 9% in urine.¹

Half-life

Averages 18 hours.¹

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹

Actions

• 
  

  Exact mechanism of action of lurasidone and other antipsychotic agents in schizophrenia unknown; efficacy may be mediated through a combination of antagonist activity at central dopamine type 2 (D₂) and serotonin type 2 (5-hydroxytryptamine [5-HT_2A]) receptors.^{1 7 9}

  
  


• 
  

  Exhibits high affinity for D₂, 5-HT_2A, and 5-HT₇ receptors and moderate affinity for α_2C-adrenergic receptors in vitro.^{1 6 7 9} Acts as a partial agonist at 5-HT_1A receptors and is an antagonist at α_2A-adrenergic receptors in vitro.^{1 6 7 9}

  
  


• 
  

  Exhibits weak affinity for α₁-adrenergic receptors and little or no affinity for histamine (H₁) receptors and muscarinic (M₁) receptors.^{1 6 7 9}

  
  

Advice to Patients

• 
  

  Importance of advising patients and caregivers that geriatric patients with dementia-related psychosis treated with antipsychotic agents are at an increased risk of death.^{1 28 39 73} Patients and caregivers also should be informed that lurasidone is not approved for treating geriatric patients with dementia-related psychosis.^{1 73}

  
  


• 
  

  Importance of informing patients and caregivers about the risk of NMS, which can cause high fever, stiff muscles, sweating, fast or irregular heart beat, change in BP, confusion, and kidney damage.¹

  
  


• 
  

  Importance of patients being aware of the symptoms of hyperglycemia and diabetes mellitus (e.g., increased thirst, increased urination, increased appetite, weakness).¹ Importance of informing patients who are diagnosed with diabetes, those with risk factors for diabetes, and those who develop hyperglycemia symptoms during treatment that they should have their blood glucose monitored at the beginning of and periodically during lurasidone treatment.¹

  
  


• 
  

  Risk of orthostatic hypotension, especially when initiating or reinitiating treatment or increasing the dosage.¹

  
  


• 
  

  Risk of leukopenia/neutropenia.¹ Importance of advising patients with a preexisting low WBC count or history of drug-induced leukopenia/neutropenia that their CBC count should be monitored during lurasidone therapy.¹

  
  


• 
  

  Risk of somnolence (i.e., sleepiness, drowsiness).¹ Importance of advising patients to exercise caution when performing activities requiring mental alertness (e.g., driving or operating hazardous machinery) until they gain experience with the drug’s effects.¹

  
  


• 
  

  Importance of avoiding alcohol during lurasidone therapy.¹

  
  


• 
  

  Importance of informing patients in whom chronic lurasidone use is contemplated of risk of tardive dyskinesia.^{1 67} Importance of advising patients to report any muscle movements that cannot be stopped to a healthcare professional.⁶⁷

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription (see Interactions) and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease, diabetes mellitus, seizures).¹

  
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 81} Importance of clinicians informing patients about the benefits and risks of taking antipsychotics during pregnancy (see Pregnancy under Cautions).^{1 81} Importance of advising patients not to stop taking lurasidone if they become pregnant without consulting their clinician; abruptly stopping antipsychotic agents may cause complications.⁸¹ Importance of advising patients not to breast-feed during lurasidone therapy.¹

  
  


• 
  

  Importance of avoiding overheating and dehydration.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Lurasidone Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	40 mg	Latuda	Sunovion
		80 mg	Latuda	Sunovion

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 10/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Latuda 80MG Tablets (SUNOVION PHARMACEUTICALS): 30/$475.98 or 90/$1,396.03

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions September 28, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Sunovion Pharmaceuticals Inc. Latuda (lurasidone hydrochloride) tablets prescribing information. Marlborough, MA; 2010 Oct.

2. Nakamura M, Ogasa M, Guarino J et al. Lurasidone in the treatment of acute schizophrenia: a double-blind, placebo-controlled trial. J Clin Psychiatry. 2009; 70:829-36. [PubMed 19497249]

3. Meyer JM, Cucchiaro J, Pikalov A et al. Differential metabolic profiles of lurasidone and olanzapine: data from a 6-week, double-blind, placebo-controlled schizophrenia trial [abstract]. Presented at the 163rd Annual American Psychiatric Association Meeting. New Orleans, LA: 2010 May 22-26. Abstract NR6-19.

4. Cucchiaro J, Pikalov A, Ogasa M et al. Safety of lurasidone: pooled analysis of five placebo-controlled trials in patients with schizophrenia. Presented at the163rd Annual American Psychiatric Association Meeting. New Orleans, LA: 2010 May 22-26. Abstract NR6-20.

5. Meltzer H, Cucchiaro J, Silva R et al. Lurasidone in the treatment of acute schizophrenia: results of the double-blind placebo-controlled PEARL 2 trial [abstract]. Presented at the 163rd Annual American Psychiatric Association Meeting. New Orleans, LA: 2010 May 22-26. Abstract NR6-15.

6. Ishiyama T, Loebel A, Cucchiaro J et al. Comparative receptor binding profile of lurasidone and other first and second generation antipsychotics [abstract]. Presented at the 163rd Annual American Psychiatric Association Meeting. New Orleans, LA: 2010 May 22-26. Abstract NR6-40.

7. Ishibashi T, Horisawa T, Tokuda K et al. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010; 334:171-81. [PubMed 20404009]

8. Citrome L. Lurasidone for schizophrenia: a review of the efficacy and safety profile for this newly approved second-generation antipsychotic. Int J Clin Pract. 2011; 65:189-210. [PubMed 21129135]

9. Meyer JM, Loebel AD, Schweizer E. Lurasidone: a new drug in development for schizophrenia. Expert Opin Investig Drugs. 2009; 18:1715-26. [PubMed 19780705]

11. Eli Lilly and Company. Zyprexa (olanzapine) tablets and Zyprexa Zydis (olanzapine) orally disintegrating tablets prescribing information. Indianapolis, IN; 2004 Sep 22.

12. Eli Lilly and Company. Lilly announces FDA notification of class labeling for atypical antipsychotics regarding hyperglycemia and diabetes. Indianapolis, IN; 2003 Sep 17. Press release.

13. Dixon L, Perkins D, Calmes C. Guideline watch (September 2009): practice guideline for the treatment of patients with schizophrenia. American Psychiatric Association. Arlington, VA; 2009 Sep. From the American Psychiatric Association website: .

14. Novartis Pharmaceuticals. Clozaril (clozapine) prescribing information. East Hanover, NJ; 2003 Dec.

15. AstraZeneca Pharmaceuticals. Seroquel (quetiapine fumarate) tablets prescribing information. Wilmington, DE; 2004 Jul.

16. Janssen Pharmaceutica. Risperdal (risperidone) tablets and oral solution prescribing information. Titusville, NJ; 2003 Oct.

17. Pfizer Inc. Geodon (ziprasidone) prescribing information. New York, NY; 2004 Aug.

18. Lewis-Hall F. Dear health care professional letter regarding class labeling for atypical antipsychotics and risk of hyperglycemia and diabetes. Princeton, NJ: Bristol-Myers Squibb Company; 2004 Mar 25. From FDA website.

19. Bess AL, Cunningham SR. Dear health care professional letter regarding class labeling for atypical antipsychotics and risk of hyperglycemia and diabetes. East Hanover, NJ: Novartis Pharmaceuticals Corporation; 2004 Apr 1. From the FDA website.

20. Eisenberg P. Dear health care professional letter regarding safety data on Zyprexa (olanzapine) – hyperglycemia and diabetes. Indianapolis, IN: Eli Lilly and Company; 2004 Mar 1. From the FDA website.

21. Macfadden W. Dear health care professional letter regarding class labeling for atypical antipsychotics and risk of hyperglycemia and diabetes. Wilmington, DE: AstraZeneca Pharmaceuticals; 2004 Apr 22. From the FDA website.

22. Mahmoud RA. Dear health care professional letter regarding class labeling for atypical antipsychotics and risk of hyperglycemia and diabetes. Titusville, NJ: Janssen Pharmaceutica, Inc; 2004. From the FDA website.

23. Clary CM. Dear health care practitioner letter regarding class labeling for atypical antipsychotics and risk of hyperglycemia and diabetes. New York NY: Pfizer Global Pharmaceuticals; 2004 Aug. From the FDA website.

24. Cunningham F, Lambert B, Miller DR et al. Antipsychotic induced diabetes in veteran schizophrenic patients. In: Abstracts of the 1st International Conference on Therapeutic Risk Management and 19th International Conference on Pharmacoepidemiology, Philadelphia, PA, 2003 Aug 21-24. Pharmacoepidemiol Drug Saf. 2003; 12(Suppl 1): S154-5.

25. American Diabetes Association; American Psychiatric Association; American Association of Clinical Endocrinologists; North American Association for the Study of Obesity. Consensus development conference on antipsychotic drugs and obesity and diabetes. Diabetes Care. 2004; 27:596-601. [PubMed 14747245]

26. Melkersson K, Dahl ML. Adverse metabolic effects associated with atypical antipsychotics. Drugs. 2004; 64:701-23. [PubMed 15025545]

27. Citrome LL, Jaffe AB. Relationship of atypical antipsychotics with development of diabetes mellitus. Ann Pharmacother. 2003; 37:1849-57. [PubMed 14632602]

28. American Psychiatric Association. Practice guideline for the treatment of patients with schizophrenia, second edition. Am J Psychiatry. 2004; 161(2 Suppl):1-56.

29. Sumiyoshi T, Roy A, Anil AE et al. A comparison of incidence of diabetes mellitus between atypical antipsychotic drugs. J Clin Psychopharmacol. 2004; 24:345-8. [PubMed 15118492]

30. Expert Group. ’Schizophrenia and Diabetes 2003’ expert consensus meeting, Dublin, 3–4 October 2003: consensus summary. Br J Psychiatry. 2004; 47(Suppl):S112-4.

31. Schering-Plough. Saphris (asenapine maleate) sublingual tablets prescribing information. Kenilworth, NJ; 2009 Aug.

32. Holt RI. Consensus development conference on antipsychotic drugs and obesity and diabetes: response to consensus statement. Diabetes Care. 2004; 27:2086-7. [PubMed 15277449]

33. Citrome L, Volavka J. Consensus development conference on antipsychotic drugs and obesity and diabetes: response to consensus statement. Diabetes Care. 2004; 27:2087-8. [PubMed 15277450]

34. Isaac MT, Isaac MB. Consensus development conference on antipsychotic drugs and obesity and diabetes: response to consensus statement. Diabetes Care. 2004; 27:2088. [PubMed 15277451]

35. Boehm G, Racoosin JA, Laughren TP et al. Consensus development conference on antipsychotic drugs and obesity and diabetes: response to consensus statement. Diabetes Care. 2004; 27:2088-9. [PubMed 15277452]

36. Barrett EJ. Consensus development conference on antipsychotic drugs and obesity and diabetes: response to Holt, Citrome and Volevka, Isaac and Isaac, and Boehm et al. Diabetes Care. 2004; 27:2089-90.

37. Fuller MA, Shermock KM, Secic M et al. Comparative study of the development of diabetes mellitus in patients taking risperidone and olanzapine. Pharmacotherapy. 2002; 23:1037-43.

38. Koller EA, Cross JT, Doraiswamy PM et al. Risperidone-associated diabetes mellitus: a pharmacovigilance study. Pharmacotherapy. 2003; 23:735-44. [PubMed 12820816]

39. US Food and Drug Administration. Information for Healthcare Professionals: Conventional antipsychotics. Rockville, MD; 2008 Jun 16. From the FDA websit

Lavoclen-4 Creamy Wash

Generic Name: benzoyl peroxide topical (BEN zoyl per OX ide)

Brand Names: Acne Treatment, Acne-Clear, Benzac AC, Benzac W, Benzashave 10, Benzashave 5, BenzEFoam, Benziq, Benziq Wash, BPO Foaming Cloths, Brevoxyl, Brevoxyl Acne Wash Kit, Brevoxyl-4 Creamy Wash Complete Pack, Brevoxyl-8 Creamy Wash Complete Pack, Breze, Clearplex, Clearskin, Clinac BPO, Desquam-E, Desquam-X 10, Desquam-X 5, Desquam-X Wash, Fostex Bar 10%, Fostex Gel 10%, Fostex Wash 10%, Inova, Lavoclen-4, Lavoclen-8, Loroxide, NeoBenz Micro, Neutrogena Acne Mask, Neutrogena On Spot Acne Treatment, Oscion, Oscion Cleanser, Oxy 10 Balance, Oxy Balance, Oxy Daily Wash Chill Factor, Oxy-10, Pacnex, PanOxyl, Panoxyl 10, Panoxyl 5, Panoxyl Aqua Gel, PanOxyl Maximum Strength Foaming Acne Wash, Persa-Gel, Seba-Gel, SoluCLENZ Rx, Triaz, Triaz Cleanser, Zaclir

What is Lavoclen-4 Creamy Wash (benzoyl peroxide topical)?

Benzoyl peroxide has an antibacterial effect. It also has a mild drying effect, which allows excess oils and dirt to be easily washed away from the skin.

Benzoyl peroxide topical (for the skin) is used to treat acne.

Benzoyl peroxide topical may also be used for purposes not listed in this medication guide.

What is the most important information I should know about Lavoclen-4 Creamy Wash (benzoyl peroxide topical)?

There are many brands and forms of benzoyl peroxide available and not all brands are listed on this leaflet.

Do not use benzoyl peroxide topical while you are also using tretinoin (Altinac, Avita, Renova, Retin-A, Tretin-X). Using these medications together could cause severe skin irritation.

Use this medication exactly as directed on the label, or as prescribed by your doctor. Do not use it in larger amounts or for longer than recommended.

Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water. Do not use benzoyl peroxide topical on sunburned, windburned, dry, chapped, irritated, or broken skin. Also avoid using benzoyl peroxide topical on wounds or on areas of eczema. Wait until these conditions have healed before using this medication.

Avoid using skin products that can cause irritation, such as harsh soaps, shampoos, or skin cleansers, hair coloring or permanent chemicals, hair removers or waxes, or skin products with alcohol, spices, astringents, or lime. Do not use other medicated skin products unless your doctor has told you to.

Benzoyl peroxide may bleach hair or fabrics. Avoid allowing this medication to come into contact with your hair or clothing.

It may take several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

What should I discuss with my healthcare provider before using Lavoclen-4 Creamy Wash (benzoyl peroxide topical)?

Do not use benzoyl peroxide topical while you are also using tretinoin (Altinac, Avita, Renova, Retin-A, Tretin-X). Using these medications together could cause severe skin irritation. FDA pregnancy category C. It is not known whether benzoyl peroxide topical will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. It is not known whether benzoyl peroxide passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use Lavoclen-4 Creamy Wash (benzoyl peroxide topical)?

Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.

Wash your hands before and after applying this medication. Shake the lotion well just before each use.

Clean and pat dry the skin to be treated. Apply benzoyl peroxide in a thin layer and rub in gently.

Do not cover the treated skin area unless your doctor has told you to.

Benzoyl peroxide topical is usually applied one to three times daily. Follow your doctor's instructions.

Benzoyl peroxide may bleach hair or fabrics. Avoid allowing this medication to come into contact with your hair or clothing.

It may take several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while using Lavoclen-4 Creamy Wash (benzoyl peroxide topical)?

Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water. Do not use benzoyl peroxide topical on sunburned, windburned, dry, chapped, irritated, or broken skin. Also avoid using benzoyl peroxide topical on wounds or on areas of eczema. Wait until these conditions have healed before using this medication.

Avoid using skin products that can cause irritation, such as harsh soaps, shampoos, or skin cleansers, hair coloring or permanent chemicals, hair removers or waxes, or skin products with alcohol, spices, astringents, or lime. Do not use other medicated skin products unless your doctor has told you to.

Avoid using sunscreen containing PABA on the same skin treated with benzoyl peroxide, or skin discoloration may occur.

Lavoclen-4 Creamy Wash (benzoyl peroxide topical) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using benzoyl peroxide and call your doctor at once if you have severe stinging or burning of your skin.

Less serious side effects may include:

• 
  

  mild stinging or burning;

  
  


• 
  

  itching or tingly feeling;

  
  


• 
  

  skin dryness, peeling, or flaking; or

  
  


• 
  

  redness or other irritation.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Lavoclen-4 Creamy Wash (benzoyl peroxide topical)?

It is not likely that other drugs you take orally or inject will have an effect on topically applied benzoyl peroxide topical. But many drugs can interact with each other. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More Lavoclen-4 Creamy Wash resources

• Lavoclen-4 Creamy Wash Side Effects (in more detail)
• Lavoclen-4 Creamy Wash Use in Pregnancy & Breastfeeding
• Lavoclen-4 Creamy Wash Drug Interactions
• Lavoclen-4 Creamy Wash Support Group
• 0 Reviews for Lavoclen-4y - Add your own review/rating

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Compare Lavoclen-4 Creamy Wash with other medications

• Acne
• Perioral Dermatitis

Where can I get more information?

• Your pharmacist can provide more information about benzoyl peroxide topical.

See also: Lavoclen-4y side effects (in more detail)

Laryng-O-Jet

Generic Name: lidocaine hydrochloride

Dosage Form: Topical Solution USP, 4%

DISPOSABLE KIT WITH LIDOCAINE HYDROCHLORIDE TOPICAL SOLUTION

FOR LARYNGOTRACHEAL ANESTHESIA

Rx Only

Laryng-O-Jet Description

Lidocaine HCl Topical Solution USP, 4% is a sterile, aqueous solution containing a local anesthetic agent and is administered topically.

Lidocaine hydrochloride is designated chemically as acetamide, 2-(diethylamino)-N-(2, 6-dimethylphenyl)-monohydrochloride, with the following structural formula:

Composition of Lidocaine HCl 4% Topical Solution

Each mL of aqueous solution contains lidocaine HCl, 40 mg, and sodium hydroxide and/or hydrochloric acid to adjust pH to 5.0 to 7.0. No preservative is added since all or part of the contents of the syringe unit is administered as a single dose and the unit should not be re-used.

Laryng-O-Jet - Clinical Pharmacology

Mechanism of Action

Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. The onset of action is rapid.

Hemodynamics

Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial pressure. These changes may be attributable to a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system. The net effect is normally a modest hypotension when the recommended dosages are not exceeded.

Pharmacokinetics and Metabolism

Lidocaine may be absorbed following topical administration to mucous membranes, its rate and extent of absorption depending upon concentration and total dose administered, the specific site of application, and duration of exposure. In general, the rate of absorption of local anesthetic agents following topical application occurs most rapidly after intratracheal administration. Lidocaine is also well-absorbed from the gastrointestinal tract, but little intact drug appears in the circulation because of biotransformation in the liver.

Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than those of lidocaine. Approximately 90% of lidocaine administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-dimethylaniline.

Studies have shown that peak blood levels of lidocaine may occur as early as 5 and as late as 30 minutes after endotracheal administration of a 4% lidocaine HCl solution.

The plasma binding of lidocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 to 4 µg of free base per mL, 60 to 80 percent of lidocaine is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein.

Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.

Studies of lidocaine metabolism following intravenous bolus injections have shown that the elimination half-life of this agent is typically 1.5 to 2 hours. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged two-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites.

Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6 µg free base per mL. In the rhesus monkey arterial blood levels of 18– 21 µg/mL have been shown to be threshold for convulsive activity.

Indications and Usage for Laryng-O-Jet

Lidocaine HCl Topical Solution, 4% is indicated for the production of topical anesthesia of the mucous membranes of the respiratory tract.

Contraindications

Lidocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type.

Warnings

LIDOCAINE HCl TOPICAL SOLUTION SHOULD BE EMPLOYED ONLY BY CLINICIANS WHO ARE WELL VERSED IN DIAGNOSIS AND MANAGEMENT OF DOSE-RELATED TOXICITY AND OTHER ACUTE EMERGENCIES THAT MIGHT ARISE AND THEN ONLY AFTER ENSURING THE IMMEDIATE AVAILABILITY OF OXYGEN, OTHER RESUSCITATIVE DRUGS, CARDIOPULMONARY EQUIPMENT, AND THE PERSONNEL NEEDED FOR PROPER MANAGEMENT OF TOXIC REACTIONS AND RELATED EMERGENCIES. (See also "ADVERSE REACTIONS" and "PRECAUTIONS.") DELAY IN PROPER MANAGEMENT OF DOSE-RELATED TOXICITY, UNDERVENTILATION FROM ANY CAUSE AND/OR ALTERED SENSITIVITY MAY LEAD TO THE DEVELOPMENT OF ACIDOSIS, CARDIAC ARREST AND, POSSIBLY, DEATH.

Lidocaine HCl Topical Solution should be used with extreme caution if there is sepsis or severely traumatized mucosa in the area of application, since under such conditions there is the potential for rapid systemic absorption.

Precautions

General

The safety and effectiveness of lidocaine depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies. Resuscitative equipment, oxygen and other resuscitative drugs should be available for immediate use. (See "WARNINGS" and "ADVERSE REACTIONS".) The lowest dosage that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects. Repeated doses of lidocaine may cause significant increases in blood levels with each repeated dose because of slow accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with the status of the patient. Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their age and physical status. Lidocaine should also be used with caution in patients with severe shock or heart block.

Careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs and the patient's state of consciousness should be accomplished after each local anesthetic injection. It should be kept in mind at such times that restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression or drowsiness may be early warning signs of central nervous system toxicity.

Since amide-type local anesthetics are metabolized by the liver, Lidocaine HCl Topical Solution should be used with caution in patients with hepatic disease. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at a greater risk of developing toxic plasma concentrations. Lidocaine HCl Topical Solution should also be used with caution in patients with impaired cardiovascular function since they may be less able to compensate for functional changes associated with the prolongation of A-V conduction produced by these drugs.

Many drugs used during the conduct of anesthesia are considered potential triggering agents for familial malignant hyperthermia. Since it is not known whether amide-type local anesthetics may trigger this reaction and since the need for supplemental general anesthesia cannot be predicted in advance, it is suggested that a standard protocol for management should be available. Early unexplained signs of tachycardia, tachypnea, labile blood pressure and metabolic acidosis may precede temperature elevation. Successful outcome is dependent on early diagnosis, prompt discontinuance of the suspect triggering agent(s) and institution of treatment, including oxygen therapy, indicated supportive measures and dantrolene (consult dantrolene sodiu m intravenous package insert before using).

Lidocaine should be used with caution in persons with known drug sensitivities. Patients allergic to para-amino-benzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross sensitivity to lidocaine.

Information for Patients

When topical anesthetics are used in the mouth, the patient should be aware that the production of topical anesthesia may impair swallowing and thus enhance the danger of aspiration. For this reason, food should not be ingested for 60 minutes following use of local anesthetic preparations in the mouth or throat area. This is particularly important in children because of their frequency of eating.

Numbness of the tongue or buccal mucosa may enhance the danger of unintentional biting trauma. Food and chewing gum should not be used while the mouth or throat area is anesthetized.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Studies of lidocaine in animals to evaluate the carcinogenic and mutagenic potential or the effect on fertility have not been conducted.

Use in Pregnancy

Teratogenic Effects

Pregnancy Category B

Reproduction studies have been performed in rats at doses up to 6.6 times the human dose and have revealed no evidence of harm to the fetus caused by lidocaine. There are, however, no adequate and well-controlled studies in pregnant women. Animal reproduction studies are not always predictive of human response. General consideration should be given to this fact before administering lidocaine to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place.

Labor and delivery

Lidocaine is not contraindicated in labor and delivery. Should Lidocaine HCl Topical Solution be used concomitantly with other products containing lidocaine, the total dose contributed by all formulations must be kept in mind.

Nursing mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when lidocaine is administered to a nursing woman.

Pediatric use

Dosages in children should be reduced, commensurate with age and body weight. See "DOSAGE AND ADMINISTRATION."

Adverse Reactions

Adverse experiences following the administration of lidocaine are similar in nature to those observed with other amide local anesthetic agents. These adverse experiences are, in general, dose-related and may result from high plasma levels caused by excessive dosage or rapid absorption, or may result from a hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient. Serious adverse experiences are generally systemic in nature.

The following types are those most commonly reported:

Central Nervous System

CNS manifestations are excitatory and/or depressant and may be characterized by lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression and arrest. The excitatory manifestations may be very brief or may not occur at all, in which case the first manifestation of toxicity may be drowsiness merging into unconsciousness and respiratory arrest.

Drowsiness following the administration of lidocaine is usually an early sign of a high blood level of the drug and may occur as a consequence of rapid absorption.

Cardiovascular System

Cardiovascular manifestations are usually depressant and are characterized by bradycardia, hypotension, and cardiovascular collapse, which may lead to cardiac arrest.

Allergic

Allergic reactions are characterized by cutaneous lesions, urticaria, edema or anaphylactoid reactions. Allergic reactions as a result of sensitivity to lidocaine are extremely rare and, if they occur, should be managed by conventional means. The detection of sensitivity by skin testing is of doubtful value.

Neurologic

The incidences of adverse reactions associated with the use of local anesthetics may be related to the total dose of local anesthetic administered and are also dependent upon the particular drug used, the route of administration and the physical status of the patient.

Overdosage

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics. See "ADVERSE REACTIONS", "WARNINGS" and "PRECAUTIONS."

The intravenous LD50 of lidocaine HCl in female mice is 26 (21–31) mg/kg and the subcutaneous LD50 is 264 (203–304) mg/kg.

Management of Local Anesthetic Emergencies

The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness after each local anesthetic administration. At the first sign of change, oxygen should be administered.

The first step in the management of convulsions consists of immediate attention to the maintenance of a patent airway and assisted or controlled ventilation with oxygen and a delivery system capable of permitting immediate positive airway pressure by mask. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be evaluated, keeping in mind that drugs used to treat convulsions sometimes depress the circulation when administered. Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, small increments of an ultra-short acting barbiturate (such as thiopental or thiamylal) or a benzodiazepine (such as diazepam) may be administered intravenously. The clinician should be familiar, prior to use of local anesthetics, with these anticonvulsant drugs. Supportive treatment of circulatory depression may require administration of intravenous fluids and, when appropriate, a vasopressor as directed by the clinical situation (e.g., ephedrine).

If not treated immediately, both convulsions and cardiovascular depression can result in hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest. If cardiac arrest should occur, standard cardiopulmonary resuscitative measures should be instituted.

Endotracheal intubation, employing drugs and techniques familiar to the clinician, may be indicated, after initial administration of oxygen by mask, if difficulty is encountered in the maintenance of a patent airway or if prolonged ventilatory support (assisted or controlled) is indicated.

Dialysis is of negligible value in the treatment of acute overdosage with lidocaine.

Laryng-O-Jet Dosage and Administration

When Lidocaine HCl Topical Solution is used concomitantly with other products containing lidocaine, the total dose contributed by all formulations must be kept in mind.

The dosage varies and depends upon the area to be anesthetized, vascularity of the tissues, individual tolerance and the technique of anesthesia. The lowest dosage needed to provide effective anesthesia should be administered. Dosages should be reduced for children and for elderly and debilitated patients.

Although the incidence of adverse effects with Lidocaine HCl Topical Solution is quite low, caution should be exercised, particularly when employing large volumes and concentrations of Lidocaine HCl Topical Solution since the incidence of adverse effects is directly proportional to the total dose of local anesthetic agent administered. For specific techniques and procedures refer to standard textbooks. The dosages below are for normal, healthy adults.

Topical Application

For laryngoscopy, bronchoscopy and endotracheal intubation, the pharynx may be sprayed with 1–5 mL (40–200 mg lidocaine HCl), i.e., 0.6–3 mg/kg or 0.3–1.5 mg/lb body weight. For local anesthesia by the transtracheal route, it may be occasionally necessary to spray the pharynx by oropharyngeal spray to achieve complete analgesia.

Maximum Recommended Dosages

Normal Healthy Adults

The maximum recommended dose of Lidocaine HCl Topical Solution, should be such that the dose of lidocaine HCl is kept below 300 mg and in any case should not exceed 4.5 mg/kg (2 mg/lb) body weight.

Children

It is difficult to recommend a maximum dose of any drug for children since this varies as a function of age and weight. For children of less than ten years who have a normal lean body mass and normal body development, the maximum dose may be determined by the application of one of the standard pediatric drug formulas (e.g. Clark's rule). For example, in a child of five years weighing 50 lbs., the dose of lidocaine HCl should not exceed 75–100 mg when calculated according to Clark's rule. The amount of Lidocaine HCl Topical Solution administered should be such that the dose of lidocaine is kept below 300 mg and in any case should not exceed 4.5 mg/kg (2.0 mg/lb) of body weight.

Directions for Use

DESCRIPTION

The Laryng-O-Jet® is a disposable kit for producing rapid, effective topical anesthesia of the interior of the larynx and trachea. The kit contains (1) a sterile, anatomically-curved plastic cannula with attached vial injector, and (2) a single-dose vial prefilled with 4 mL of a 4% sterile aqueous solution of lidocaine hydrochloride. Medication, cannula and fluid pathway are sterile in original, unopened package. The kit is designed for one-time use only. After use, it may be discarded without disassembly.

Figure 1. Assembled Laryng-O-Jet® system showing the location and direction of jet openings.

USE

The Laryng-O-Jet® Kit is used to instill a jet spray of lidocaine hydrochloride topical solution into the interior of the larynx and trachea for local anesthesia in the unconscious patient just prior to endotracheal intubation. This form of application also is effective as a final stage of topical anesthesia in the conscious patient (after initial use of an atomizer spray or other appropriate technique for applying topical anesthetic to the pharynx and epiglottis) prior to laryngeal or tracheobronchial endoscopic procedures.

DIRECTIONS

Use Aseptic Technique

DO NOT ASSEMBLE UNTIL READY TO USE

IMPORTANT: Use of the Laryng-O-Jet® Kit requires strict observance of precautions appropriate to use of topical anesthesia in the respiratory tract.

For Use Prior to Intubation During Anesthesia Induction (Unconscious Patient):

1. Open kit following peel pouch directions.


2. Remove vial and vial injector from bag.


3. Aseptically remove vial and vial injector caps and insert vial into injector.


4. Rotate vial about three turns clockwise or until resistance is felt. DO NOT PUSH VIAL INTO INJECTOR; THIS MAY CAUSE MISALIGNMENT. Needle will then be in contact with medication (Fig. 1). Assembled unit should remain in field until laryngoscopy has been completed.


5. Before instillation, manually ventilate the patient with 5 or 6 deep breaths of 100% oxygen (denitrogenate with at least 5 minutes of high flow semi-closed 100% oxygen administration in patients with low cardio-respiratory, circulatory, or hematologic reserve).


6. Predetermine dose (volume) of anesthetic to be instilled and expel excess solution.


7. After hypnosis and muscle relaxation have developed fully and oxygenation has been accomplished as above, perform laryngoscopy in conventional manner. See Fig. 2.
   

   Figure 2. Laryngoscopist's view showing cannula in place in adult larynx and trachea, with black guide mark just proximal to cords.

   
   
   
   

8.

Hold injector in manner of holding a pen, and insert tip of cannula between vocal cords and into trachea to the proper depth for instillation of local anesthetic. The black guide mark is positioned just proximal to vocal cords. At this depth, interior of larynx will be bathed with anesthetic solution from upper jet orifices and entire tracheal wall by lower jet openings. (NOTE: Black mark on cannula shaft indicates approximate depth for insertion in most normal patients without touching carina with distal tip.) Caution and gentleness during insertion should be observed and the cannula advanced a proportionately shorter distance in those persons suspected of having a high tracheal bifurcation or tracheobronchial anomaly.

9.

With cannula at proper depth, depress syringe plunger rapidly to produce a jet-like instillation for bathing walls of larynx and trachea. NOTE: Depression of syringe plunger too slowly may fail to eject solution with sufficient velocity to reach all parts of the larynx and trachea.

10.

Withdraw unit and discard.

11.

Proceed with intubation.

For Use in Endoscopic Procedures to Supplement Initial Atomizer Spray of Local Anesthetic (Conscious Patient):

1. Predetermine dose and assemble unit as in steps 1, 2, 3, 4 and 6 (above).


2. Before instillation apply an initial local anesthetic to the pharynx and epiglottis using an atomizer spray or other appropriate technique.


3. Follow steps 8, 9 and 10 (above) for instillation.


4. Proceed with desired laryngeal or tracheobronchial endoscopy.

How is Laryng-O-Jet Supplied

In unit use packages containing one sterile disposable laryngotracheal cannula with attached vial injector, and one disposable single dose vial prefilled with sterile, aqueous solution of lidocaine hydrochloride.

        STOCK NO. 6300        4 mL        4%        Laryng - O - Jet®        NDC 0548-6300-00

Twenty-five unit use packages per carton.

Manufactured under Laryng-O-Jet® System.

Store at controlled room temperature 15° to 30°C (59° to 86°F)[see USP].

INTERNATIONAL MEDICATION SYSTEMS, LIMITED

SOUTH EL MONTE, CA 91733, U.S.A.

An Amphastar Pharmaceuticals Company

6963000N

REV. 9-04

Laryng-O-Jet  lidocaine hydrochloride  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0548-6300 Route of Administration TOPICAL DEA Schedule

INGREDIENTS Name (Active Moiety) Type Strength Lidocaine Hydrochloride (Lidocaine) Active 40 MILLIGRAM  In 1 MILLILITER Sodium Hydroxide Inactive   Hydrochloric Acid Inactive   Water Inactive

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0548-6300-00 25 SYRINGE In 1 CARTON contains a SYRINGE 1 4 mL (MILLILITER) In 1 SYRINGE This package is contained within the CARTON (0548-6300-00)

Revised: 05/2006International Medication Systems, Limited

More Laryng-O-Jet resources

• Laryng-O-Jet Use in Pregnancy & Breastfeeding
• Laryng-O-Jet Support Group
• 22 Reviews for Laryng-O-Jet - Add your own review/rating

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