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LOFLAZEPATE

ClassLOFLAZEPATE commonly prescribed forHow LOFLAZEPATE worksHow long until LOFLAZEPATE worksNotable Side EffectsLife Threatening Side Effectsweight gainsedationWhat to do about LOFLAZEPATE side effectsusual dosage rangeDosage Formslong term usehabit formingRenal ImpairmentHepatic ImpairmentCardiac ImpairmentElderlyChildren and AdolescentsPregnancyBreast Feeding

THERAPEUTICS

Class

  • Benzodiazepine (anxiolytic)

LOFLAZEPATE commonly prescribed for

(Bold for FDA approved)

• Anxiety, tension, depression, or sleep disorder in patients with neurosis
• Anxiety, tension, depression, or sleep disorder in patients with psychosomatic disease
• Catatonia

How LOFLAZEPATE works

• Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex

• Enhances the inhibitory effects of GABA

• Boosts chloride conductance through GABA-regulated channels

• Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders

How long until LOFLAZEPATE works

• Some immediate relief with first dosing is common; can take several weeks with daily dosing for maximal therapeutic benefit

SIDE EFFECTS

Notable Side Effects

• Sedation, fatigue, depression

• Dizziness, ataxia, slurred speech, weakness

• Forgetfulness, confusion

• Hyperexcitability, nervousness

• Rare hallucinations, mania

• Rare hypotension

• Hypersalivation, dry mouth

Life Threatening Side Effects

• Respiratory depression, especially when taken with CNS depressants in overdose

• Rare hepatic dysfunction, renal dysfunction, blood dyscrasias

weight gain

unusual

unusual

sedation

not usual

not usual

What to do about LOFLAZEPATE side effects

• Wait

• Wait

• Wait

• Lower the dose

• Take largest dose at bedtime to avoid sedative effects during the day

• Switch to another agent

• Administer flumazenil if side effects are severe or life-threatening

DOSING AND USE

usual dosage range

• 1 mg once or twice a day

Dosage Forms

• Tablet 1 mg, 2 mg

long term use

• Risk of dependence, particularly for treatment periods longer than 12 weeks and especially in patients with past or current polysubstance abuse

habit forming

• Patients may develop dependence and/or tolerance with long-term use

SPECIAL POPULATIONS

Renal Impairment

• Drug should be used with caution

Hepatic Impairment

• Drug should be used with caution

Cardiac Impairment

• Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction

Elderly

• Drug should be used with caution

• Should begin with lower starting dose

Children and Adolescents

• Safety and efficacy have not been established

• Benzodiazepines are often used in children and adolescents, especially short-term and at the lower end of the dosing scale

• Long-term effects of loflazepate in children/ adolescents are unknown

• Should generally receive lower doses and be more closely monitored

Pregnancy

Possible increased risk of birth defects when benzodiazepines are taken during pregnancy

• Because of the potential risks, loflazepate is not generally recommended as treatment for anxiety during pregnancy, especially during first trimester

• Drug should be tapered if discontinued

• Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects

• Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy

• Seizures, even mild seizures, may cause harm to the embryo/fetus

Breast Feeding

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed

• Effects on infant have been observed and include feeding difficulties, sedation, and weight loss

Based on data Published online by Cambridge University Press

Compiled by Dr. Jash Ajmera