White powder filled in green-white capsule, DOMAR and 5 are printed in black.
Each capsule of Domar contains Pinazepam 5 mg.
Chemical formula: 7-chloro-1-propargyl-5-phenyl-3-H-1,4 benzodiazepin-2(1H)-one.
Pharmacology: Pharmacodynamics: Pinazepam is a psychotropic substance of the benzodiazepines class, which act as depressants of the central nervous system (CNS), and benzodiazepine receptor agonists. They have been shown to form a component of a functional supramolecular unit known as the benzodiazepine - GABAA receptor - chloride ionosphere complex, which resides on neuronal membranes. Activation of the GABA receptor results in the opening of the chloride channel, allowing the flow of chloride ions into the neuron. This results in hyperpolarization and inhibition of the activity of the neurons, producing the anxiolytic, hypnotic, anticonvulsant, and muscle relaxant effect and may result in anterograde amnesia.
Pharmacokinetics: Pinazepam is well absorbed from the gastrointestinal tract. Following the oral administration, peak plasma concentration is reached within 2 to 3 hours. Pinazepam is mainly metabolized by n-dealkylation and hydroxylation into the active metabolites desmethyldiazepam and oxazepam. Their half-life are 40 to 120 hours and 5 to 15 hours, respectively. The inactive metabolite is 3-hydroxypinazepam. The half-life of Pinazepam is approximately 10 to 15 hours.
Adults: 5-10 mg, 2-3 times a day or as prescribed by the physician.
Elderly or severe physical disorders: The dosage should be reduced.
Children: Use as prescribed by the physician.
Symptoms: Drowsiness, confusion, slurred speech, shakiness, seizures, slow heartbeat, staggering, weakness, decreased reflexes, coma and troubled breathing.
Treatment: Decrease absorption: If the patient is conscious (and not at risk of becoming lethargic, comatose, or convulsing based on ingestion), emesis should be induced mechanically or with emetics; also, activated charcoal may be administered orally to increase clearance as well as decrease absorption of Pinazepam.
If the patient is unconscious, gastric lavage may be performed.
Treatment with specific antidote: Intravenous fluids may be administered to promote diuresis and enhance elimination.
Oxygen should be administered if respiration is depressed. Flumazenil, a specific benzodiazepine receptor antagonist, may be administered to reverse sedative effects of benzodiazepines. Patients must be closely monitored as flumazenil may precipitate seizures, especially in patients who have been using benzodiazepines for a long time or who have co-ingested a cyclic antidepressant. Because of the risk of seizure induction, flumazenil use is not recommended in epileptic patients who have been treated with benzodiazepines.
Carefully read the instructions in the product information supplied with flumazenil before use. Hypotension may be controlled, if necessary, by intravenous administration of vasopressors such as dopamine, norepinephrine, or metaraminol. Respiration, pulse, and blood pressure should be monitored.
Contraindication use as prescribed by the physician: Do not use in the patients allergic to this drug.
Do not use in patients with acute narrow angle glaucoma.
Do not use in patients with myasthenia gravis.
Do not use during pregnancy.
Do not use in patients with severe respiratory function impairment or sleep apnea.
Do not use in patients with severe hepatic function impairment.
May be habit forming, use as prescribed by the physician.
Should be used with special caution in case of breastfeeding, renal function impairment, open angle glaucoma, porphyria or history of porphyria, alcoholism and psychiatric disorders e.g. psychosis, mental depression, etc., including patient with history of drug or narcotics addiction.
Should be used with special caution in case of concomitant with other drugs that may increase or decrease the function of enzyme metabolized Benzodiazepines group. Consult with the physician in case of concomitant use.
Should be used with special caution with the patients who allergic to Benzodiazepines group.
Should not be used for prolonged periods due to narcotics addiction unless directed by the physician and consult with the physician before discontinuing medication because taper dose is needed in order to avoid withdrawal syndrome.
Should not be used concomitantly with other CNS depressant including alcohol or other product containing alcohol.
May cause drowsiness, the patient should not drive vehicles or operate machinery or any risk working.
May cause blood cell, hepatic and renal disorders.
If symptoms of insomnia, hallucinations, behavior changes, muscle weakness or fever occur, stop using Pinazepam immediately and consult a physician.
If any drug allergy or severe adverse drug reaction occur, stop using Pinazepam immediately and consult a physician or pharmacist.
Use in Children and the Elderly: Paradoxical reaction may occur in children and elderly.
The most frequent undesirable effects caused by the CNS depressant activity are drowsiness, ataxia, muscle weakness, confusion, dizziness, palpitation, tachycardia. Anterograde amnesia may also occur. GI irritation and skin reactions have been reported.
The following drugs should be taken with caution in combination with Pinazepam: Alcohol or CNS depressants. CNS depressant effects may be potentiated and the risk of apnea may be increased.
Medications that inhibit the cytochrome P450 enzymes such as oral contraceptives, cimetidine, erythromycin, fluoxetine, ketoconazole, propranolol, metoprolol. These drugs inhibit the hepatic metabolism which may result in a longer half-life of pinazepam and n-desmethyldiazepam.
Medications that stimulate the cytochrome P450 enzymes such as rifampin. These drugs increase the hepatic metabolism which may result in a shorter half-life of pinazepam and n-desmethyldiazepam.
Store in a cool, dry place (below 30°C) and protect from light.
Shelf life: PVC/aluminium blister: 3 years.
Plastic bottle: 3 years.
N05BA14 - pinazepam ; Belongs to the class of benzodiazepine derivatives anxiolytics. Used in the management of anxiety, agitation or tension.
Sign Out
