CLONAZEPAM

BRANDS: Klonopin
CLASS: Benzodiazepine (anxiolytic, anticonvulsant)
COMMONLY PRESCRIBED FOR: Panic disorder, Myoclonic seizure, Absence seizure,
acute mania, Acute psychosis, Insomnia, Catatonia.
MECHANISM OF ACTION:

 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 seizure disorders
 Inhibitory actions in cerebral cortex may provide therapeutic benefits in seizure
disorders

HOW LONG DOES IT TAKE TO WORK: Some immediate relief with first dosing is
common; can take several weeks with daily dosing for maximal therapeutic benefit.

SIDE EFFECTS: Sedation, fatigue, depression, dizziness, ataxia, slurred speech, weakness,
forgetfulness, confusion, hyperexcitability, nervousness, hypersalivation, dry mouth.
DANGEROUS SIDE EFFECTS: Respiratory depression, esp. when taken with CNS
depressants in overdose, grand mal seizures, weight gain, sedation.
Long term use of BDZ receptors may lead to development of dependance, tolerance and
withdrawal.

USUAL DOSAGE RANGE :0.125mg, 0.25mg, 0.5mg, 1mg, 2mg

Seizures: Dependant on individual response of patient, upto 20mg/day
Panicdisorder: 0.5-2mg/day either as divided doses or once at bedtime

TOXICITY: Ingestion of up to 2000 mg diazepam has resulted in only minor toxicity.

DOSE ADJUSTMENTS:

Abrupt Withdrawal: Simultaneous substitution of another anticonvulsant should be

considered when gradually withdrawing this drug.

BLACK BOX WARNINGS:

Concomitant use of benzodiazepines and opioids may result in profound respiratory
depression, coma, and death; administer concomitantly when there are no alternative options;
limit dosages and durations to minimum required; monitor for signs and symptoms of
respiratory depression and sedation.

PHARMACOKINETICS:

Absorption: Bioavailability: 90%, Onset: 20-40 min, Peak plasma time: 1-4 hr; 5-7 days
(steady state)

Distribution: Protein bound: 85%, Vd: 1.5-3 L/kg

Metabolism: Metabolized by CYP3A4 (minor), glucuronic acid conjugation, Metabolites:
Inactive
Elimination: Half-life: 17-60 hr (adults); 22-33 hr (children)
Excretion: Urine

DRUG INTERACTIONS: Increased depressive effects when taken with other CNS
depressants.
Inhibitors of CYP450 3A4 may affect the clearance of Clonazepam, but dosage adjustment
usually not necessary.
Flumazenil may precipitate seizures and should not be used in patients treated for seizure
disorders with clonazepam
Use of clonazepam with valproate may cause absence status

DO NOT USE:
If patient has angle-closure glaucoma
If patient has severe liver disease
If there is a proven allergy to clonazepam or any BDZ

SPECIAL POPULATIONS:

Renal Impairment: Dose should be reduced

Hepatic Impairment: Dose should be reduced
Cardiac Impairment: BDZ have been used to treat anxiety associated with acute myocardial
infarction
Elderly: Should receive lower doses and be monitored
Pregnancy: Possible increased risk of birth defects when BDZ taken during pregnancy
Due to potential risks, clonazepam is not generally recommended as treatment for anxiety
during pregnancy, especially during the first trimester
Drug should be tapered if discontinued
Infants whose mothers received a BDZ late in pregnancy may experience withdrawal effects
Neonatal flaccidity reported in infants whose mothers took a BDZ during pregnancy
Breast Feeding:
Some drug is found in mother’s breast milk
Effects on infant have been observed and include feeding difficulties, sedation, and weight
loss.

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of
the next dose, skip the missed dose. Take your next dose at the regular time. Do not double
the dose to catch up.

STORAGE: Store at room temperature away from light and moisture. Do not store in the
bathroom. Keep all medications away from children and pets.Do not flush medications down
the toilet or pour them into a drain unless instructed to do so. Properly discard this product
when it is expired or no longer needed.