TENFREE ( Alprazolam )

ALPRAZOLAM

Alprazolam belongs to Benzodiazepine group of Drugs.

It is a short acting Benzodiazepine which acts mainly as anti-anxiety Drug.

Mechanism of Action -:

It acts by preferentially on Mid Brain (which maintains wakefulness) & Limbic system (thought & mental function).

It acts by binding with BZOs binding site located on GABAA receptor CT channel complex thus potentiate  the action of GABA.

It is responsible for inhibitory neurotransmission in the CNS.

GABA slows down nerve cell activity to cause relaxation and decrease Nerve excitement.

Pharmacokinetics -:

Alprazolam is administered Orally and is rapidly absorbed following Oral dose.

Peak conc. In the Plasma occurs in 1-2 hours following administration.

Drug is widely distributed in the body, may cause Cross placenta and distribute into the Breast Milk.

Bioavailability is = 88%

It is 80-90% bound to Plasma Protein.

It is metabolized in the Liver by Cytochrome P450 3A mainly into two metabolites,

£- Hydroxy Alprazolam

It is metabolized in the Liver by Cytochrome P450 3A mainly into two metabolites,

1. £- Hydroxy Alprazolam - Active Metabolite

2. Benzophenon -  inactive Metabolite.

Plasma Half life is 12-15 hours.

It is excreted in Urine as unchanged Drug &  Metabolite.

Adverse effects -:

Most frequently reported are Drowsiness, co-ordination difficulties and Dizziness.

Other less frequently observed effects are,

In relation to Brain- Headache, seizures, irritability, sleep disturbance, euphoria & mental confusion.

In relation to Heart- hypotension, tachycardia, tachycardia, palpitations.

In relation to blood- decrease Hb and hematocrit

Dependence may develop after prolonged use.

Contraindications -:

Hypersensitivity to Alprazolam or other BZDs.

Pregnancy and Lactation

Infants

In patients with narrow angle glaucoma.

Drug interactions -:

Co-administration of alprazolam with potent inhibitors of cytochrome P450 3A like azole like agents is not recommended.

It produces additive CNS depressant effects when co-administered with other psychotropic medications, anticonvulsants, antihistamines, ethanol, antidepressants and other drugs with themselves produce CNS depression.

INDICATIONS (USES) -:

ANXIETY DISORDERS

PANIC DISORDERS

DEPRESSION