Diazepam
Diazepam is a 1,4-benzodiazipine. A substituent in the 7th position such as halogen or a nitro group is required for its sedative, hypnotic activity. Benzdiazipines are the most widely used anxiolytic drugs. The benzodiazipines are more effective and safer. They have largely replaced barbiturates and meprobamate in the treatemnt of anxiety. Diazepam is also useful in reducing muscletone in spasticity and as an anticonvulsant.
Primary Characteristics
It is of Synthetic origin and belongs to Benzodiazepine.
It belongs to Chloride Channel Potentiater (GABA operated) pharmacological group on the basis of mechanism of action and also classified in Benzodiazepine pharmacological group.
Molecular Weight: 284.7 · pKa: 3.7 · Solubility in Water: very slight · Solubility in Alcohol: 1 in 25 · Non-proprietary name: Diazepam.
Pharmacokinetics
Absorption: Diazepam has an oral bioavailability is 50% (±50%).
Distribution: Diazepam has a volume of distribution is 1.1 l/kg. plasma protein binding is 98-99%.
Elimination: it is metabolised via Hepatic, plasma half-life is 30 hr, renal excretion is major.
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Indications
Diazepam is primarily indicated in conditions like Agitation, Alcohol withdrawal, Amnesia induction, Anxiety, Chloroquine overdose, Dyspnoea associated with anxiety in palliative care, Flare with initial gonadorelin therapy, Herpes zoster, Insomnia, Minor surgical and medical procedures, Muscle spasm (acute), Muscle spasm in palliative care, Muscular spasm, Partial seizures, Premedication, Sedation induction, Severe acute anxiety, Severely emetognic chemotherapy, Status epilepticus, Tetanus, Tonic-clonic seizures, Treatment of acute migraine attacks.
Diazepam is also indicated for secondary conditions like Acute diarrhoea, All forms of epilepsy, Bone pain in neoplastic disease, Hypercalcaemia of malignancy, Influenza A, Muscle spasm of varied aeitology, Myoclonus, Prevention and treatment of corticosteroid-induced osteoporosis.
Contraindications
Diazepam is contraindicated in conditions like Myasthenia gravis.
Dosage
Diazepam's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 5 – 20 mg | — | — | IV inj | It is given for premedication before general anaesthesia and for sedadion during surgical procedure. |
| 5 – 20 mg | — | Every 12h | Oral | for alcohol withdrawal syndrome. |
| 5 – 15 mg | — | — | Oral | At bed time for insomnia. |
| 8.5 mg | 8.5 mg | — | Oral | Up to 60 mg. It is given for muscle spasm. |
| 16 mg | 16 mg | Every 8h | Oral | For severe anxity. |
| 31 mg | 31 mg | — | Oral | It is used in a vearity of seizures in divided doses. |
| 6 mg | 6 mg | Every 3h | PO,PR,IM,Slow IV | or frequency may be increased to 3 times a day. |
| 500 ug/kg | 500 ug/kg | Every 12h | rectal solution | To a maximum of 30mg. |
| Paediatric Dosage (20kg) | ||||
| 0.25 mg/kg | 0.25 mg/kg | — | Intra Rectal | Single Dose |
| 0.25 mg/kg | 0.25 mg/kg | Every 24h | Oral | |
| 0.25 | 0.25 | — | Slow IV | Single Dose |
| Neonatal Dosage (3kg) | ||||
| 0.25 mg/kg | 0.25 mg/kg | — | Slow intravenous | Single dose |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Diazepam produces potentially life-threatening effects which include Blood dyscrasias, Respiratory arrest, Cardiac Arrest . Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Diazepam are Coma, Reduced reflexes, Apnea, Drowsiness, Confusion , Areflexia, Cardiorespiratory depression.
Diazepam is known to cause more or less tolerable side effects which are usually transient. These include Anxiety, Ataxia, Blurred vision, Changes in libido , Confusion, Constipation , Depression, Diplopia, Dizziness, Dysarthria , Euphoria, Excitement, Faintness , Fatigue, Flushing, Hallucination , Headache, Hematuria, Hypoactivity , Hypotension , Impairment of memory, Insomnia, Muscle weakness, Nausea, Pain at injection site, Phlebitis , Poor appetite, Skin rashesX, Sleep disturbance, Slurred speech, SomnolenceX, Tachycardia, Tremor, Urinary retensionX, VertigoX.
Warnings / Precautions
Interference in Pathology
Diazepam may interfere in the diagnosis of Slight reddish coloration in Ferrocitrate paper strip test for Levodopa .
Available Brands
Storage Conditions
Drug Classification
- 1.1.3 — preoperative medication and sedation
- 2.5 — Anticonvulsants and Antiepileptics
- 3.20 — Muscle relaxants and cholinesterase inhibitors
- 4.24.3 — Drugs used in anxiety and sleep disorders