| Alprazolam Pharmacology |
| Alprazolam |
| About Alprazolam |
| Benzodiazepine derivative, Anti anxiety. |
| Mechanism of Action of Alprazolam |
| Alprazolam mainly acts on Limbic system and ascending reticular formation in the CNS and binds to the BZD receptor. The binding will facilitates GABA mediated chloride channel opening and produce hyperpolarisation. This will produce an increase in the concentration of the inhibitory neurotransmitter GABA and increase in chloride ions and decreases firing rate of neuron. This in turn alters normal functions of the body. |
| Pharmacokinets of Alprazolam |
| Absorption: It is well absorbed after oral administration. Distribution: It is distributed widely in the body in protein bound form. Metabolism: It is metabolised to active and inactive metabolite in the liver. Excretion: Drug is excreted in urine. |
| Onset of Action for Alprazolam |
| 15 – 30 minutes |
| Duration of Action for Alprazolam |
| 12 – 16 hours |
| Half Life of Alprazolam |
| 12 -15 hours |
| Side Effects of Alprazolam |
| 1.Ataxia 2.Drowsiness 3.Light headedness 4. Slurred speech 5.Nausea 6.Constipation or diarrhoea 7.Tremor 8.Dependence 9.Anorexia 0.Confusion 11.Light headedness 12.Mood changes 13.Muscle rigidity 14.Amnesia |
| Contra-indications of Alprazolam |
| 1.Hypersensitivity to Benzodiazepines 2.Acute angle closure glaucoma |
| Special Precautions while taking Alprazolam |
| 1.Renal impairment 2.Hepatic impairment 3.Pulmonary insufficiency 4.Drug abuse 5.Bipolar disorder 6.Driving vehicles and operating machines and people involving any other dangerous activities |
| Pregnancy Related Information |
| Contraindicated |
| Old Age Related Information |
| Use with caution |
| Breast Feeding Related Information |
| Contraindicated |
| Children Related Information |
| Contraindicated NEONATES- contraindicated |
| Indications for Alprazolam |
| 1.For the short-term management of anxiety, 2.Treatment of Panic disorder. |
| Interactions for Alprazolam |
| Alcohol & other CNS depressants: Enhanced CNS effects. Aminophylline: Antagonizes the sedative effect. Cimetidine, Oral contraceptives, Disulfiram, Fluoxetine, Isoniazid, Ketoconazole, Metoprolol, Propoxyphene, Propranolol, Valproic Acid: Elimination of alprazolam decreased due to inhibition of hepatic metabolism leading to enhanced activity. Digoxin: Increase in serum concentration of Digoxin. Imipramine & Desipramine: Enhanced activity of these drugs. Levodopa: Decrease in antiparkinsonism efficacy. Rifampicine: Decreases efficacy. |
| Typical Dosage for Alprazolam |
| Adult: Anxiety: 0.25 – 0.5 mg every 8 hours in a day. Depending on the severity of the disease the dose can be gradually increased every 3 or 4 days. Maximum dose: 4 mg / day in divided dose. Anxiety with depression: 0.5 mg every 8 hours in a day Maintenance dose: 1.5 – 4.5 mg/ day in divided dose Panic disorder: starting dose: 1.5 mg /day in 3 divided dose. Depending on the severity of the disease the dose can be gradually increased every 3 or 4 days. Children: Not recommended |
| Schedule of Alprazolam |
| H |
| Storage Requirements for Alprazolam |
| The drug should be kept at 15 – 30 degree C in a tightly closed container. Keep out of the reach of children |
| Effects of Missed Dosage of Alprazolam |
| Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. |
| Effects of Overdose of Alprazolam |
| Give supportive measures and symptomatic treatment. Flumazenil can be given as antagonist. Hypotension can be treated with vasopressors.If the patient is conscious induce emesis followed by charcoal administration |