Benzodiazepines: Alprazolam, Diazepam, Lorazepam, and Clonazepam
A clinical pharmacology reference on the most commonly abused benzodiazepines in India — their salt names, mechanisms, side effects, and signs of abuse.
Part 3: Benzodiazepines — Alprazolam, Diazepam, Lorazepam, and Clonazepam
Clinical Reference for Healthcare Professionals.
1. Alprazolam
| Field | Detail |
|---|---|
| INN / Salt | Alprazolam |
| Drug Class | Triazolobenzodiazepine (Short-acting) |
| Schedule | Schedule H1 |
| Indian Brands | Alprax, Restyl, Anxit, Trika |
| Legitimate Uses | Panic disorder, generalized anxiety disorder |
Mechanism of Action
Alprazolam binds to the benzodiazepine site on the GABA-A receptor, enhancing the effect of the inhibitory neurotransmitter GABA. This increases chloride ion conductance, hyperpolarizing neurons and reducing neuronal excitability. The rapid onset and high potency make it the most abused benzodiazepine in India.
Why It Is Abused
Its extremely fast onset (15-30 minutes orally) produces a rapid “wave” of relaxation, disinhibition, and euphoria. It is also commonly used to potentiate the effects of opioids and alcohol, or to “come down” from stimulant binges.
Side Effects & Dangers
- Amnesia: Severe anterograde amnesia (blackouts).
- Paradoxical Rage: Can cause extreme aggression, especially in younger users.
- Fatal Withdrawal Seizures: Abrupt discontinuation after chronic use triggers grand mal seizures.
- Rapid Tolerance: The “high” fades quickly, driving dose escalation.
2. Diazepam
| Field | Detail |
|---|---|
| INN / Salt | Diazepam |
| Drug Class | 1,4-Benzodiazepine (Long-acting) |
| Schedule | Schedule H1 |
| Indian Brands | Calmpose, Valium, Paxum |
| Legitimate Uses | Anxiety, muscle spasm, alcohol withdrawal, seizures, pre-anesthetic |
Mechanism of Action
Same GABA-A receptor enhancement as Alprazolam, but with a much longer half-life (20-100 hours including active metabolites). This makes it less “euphoric” acutely but useful as a tapering agent for benzodiazepine detoxification.
Why It Is Abused
Diazepam is often obtained more easily than Alprazolam. Its long duration produces a sustained, mellow sedation. It is a common drug of choice in polydrug abuse (combined with alcohol or opioids).
Side Effects & Dangers
- Oversedation: Due to long-acting metabolites, sedation can persist for days.
- Drug Accumulation: In the elderly or those with liver disease, dangerous buildup occurs.
3. Lorazepam
| Field | Detail |
|---|---|
| INN / Salt | Lorazepam |
| Drug Class | 3-Hydroxybenzodiazepine (Intermediate-acting) |
| Schedule | Schedule H1 |
| Indian Brands | Lopez, Ativan, Larpose |
| Legitimate Uses | Anxiety, insomnia, status epilepticus, catatonia, pre-anesthetic |
Mechanism of Action
Lorazepam enhances GABA-A activity. Unlike Diazepam, it does NOT produce active metabolites (it undergoes direct glucuronidation). This makes it the safest benzodiazepine for patients with liver impairment, but it is still highly abusable.
Why It Is Abused
The rapid onset and potent anxiolytic effect make it valuable for immediate relief. In psychiatric settings, it is sometimes diverted from hospital stock.
Side Effects & Dangers
- Respiratory Depression: Especially lethal when combined with opioids or alcohol.
- Cognitive Decline: Long-term use is linked to increased dementia risk.
4. Clonazepam
| Field | Detail |
|---|---|
| INN / Salt | Clonazepam |
| Drug Class | 7-Nitrobenzodiazepine (Long-acting) |
| Schedule | Schedule H1 |
| Indian Brands | Rivotril, Epitril, Clonotril, Lonazep |
| Legitimate Uses | Epilepsy (petit mal, myoclonic seizures), panic disorder |
Mechanism of Action
Clonazepam acts on GABA-A receptors with potent anticonvulsant properties. It has a long half-life (18-50 hours) and high potency.
Why It Is Abused
Clonazepam produces a longer, more sustained sedation than Alprazolam. It is popular in polysubstance abuse settings and is frequently combined with opioids. Its anticonvulsant properties are sometimes exploited by other drug abusers to prevent seizures during their withdrawal from other substances.
Side Effects & Dangers
- Ataxia & Impaired Coordination: High risk of falls and accidents.
- Severe Withdrawal: Must be tapered over months. Abrupt cessation triggers seizures.
Next: Part 4: Z-Drugs and Sedatives — Zolpidem, Zopiclone, Nitrazepam
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