Pharmacology Guide
Anti-Anxietals
Last Updated:
Buspirone (Buspar) | Lorazepam (Ativan) | Sertraline (Zoloft) | Diazepam (Valium) | Alprazolam (Xanax)
Buspirone |
Buspar |
Mechanism of Action |
The Mechanism of Action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. |
Therapeutic Use |
Short-term symptomatic relief of excessive anxiety in patients with generalized anxiety disorder (psychoneurotic disorder). |
Absorption |
Buspirone is rapidly and almost completely absorbed after oral administration. Peak plasma levels in 40 to 90 minutes after a single 20 mg dose. |
Metabolism |
Buspirone is extensively metabolised in the liver. Metabolic sites in the liver are saturated by buspirone so that higher doses yield more unchanged buspirone. |
Half-life |
2 to 3 hours |
Average Daily Dose (adult) |
The recommended initial dose is 5 mg 2 to 3 times daily. |
Adverse Effects |
Dizziness, headache, drowsiness, lightheadedness, insomnia, fatigue, nervousness, decreased concentration, excitement, depression, confusion, nightmares/vivid dreams, anger/hostility. Infrequently depersonalization, noise intolerance, euphoria/feeling high, dissociative reaction, fear, loss of interest, dysphoria, hallucinations, seizures, suicidal thoughts. Rarely, slurred speech, claustrophobia, cold intolerance, stupor, psychosis. |
Drug Interaction |
Buspirone is highly bound to serum proteins and may displace other medicines. A slight increase (9%) has been noticed with digoxin. Similarly, buspirone possibly increased Cmax and AUC of nordiazepam by approximately 20%.
Buspirone increases serum haloperidol concentration. Raised blood pressure has been noticed in patients taking both buspirone and MAO-inhibitors.
Data from the controlled clinical trials with over 700 patients suggests safe co-administration of buspirone and analgesics, antihistamines, sedative-hypnotics, contraceptives, and antihypertensives. Diazepam, but not clorazepate, together with buspirone resulted in increased sedation.
The concomitant use of CYP3A inhibitors increases buspirone bioavailability, e.g. itraconazole to 19-fold, erythromycin and diltiazem to 6-fold, verapamil to 3 fold. The concomitant use of these drugs with buspirone should be avoided or buspirone dose reduced accordingly.
Potent CYP enzyme inducers may decrease the bioavailability of buspirone. Rifampicin has decreased buspirone bioavailability to 10% from control values. |
Contraindication |
Buspirone is contraindicated in patients with severe hepatic or severe renal impairment, patients with hypersensitivity to buspirone, myasthenia gravis, acute narrow-angle glaucoma, severe liver and kidney dysfunction, and/or pregnancy and breast-feeding. |
|
Ativan |
Mechanism of Action |
Like all drugs in this chemical family, (i.e. benzodiazepines), lorazepam enhances the action of the inhibitory neurotransmitter GABA by acting at the GABAA receptor. |
Therapeutic Use |
To relieve (or prevent) anxiety, relax muscles and to treat insomnia. |
Absorption |
Well absorbed after oral administration. Reaches peak plasma level in 1-2 hours and peak effect in 1-6 hours. |
Metabolism |
Conjugation with glucuronic acid in liver. |
Half-life |
10-20 hours |
Average Daily Dose (adult) |
2-6 mg (orally) |
Adverse Effects |
Dizziness, ataxia, drowsiness, tolerance, physical dependence, confusion, amnesia (memory loss). |
Drug Interaction |
Additive sedation with other depressants such as alcohol. Smokers may require higher doses. |
Contraindication |
Known allergy. Other side effects not listed above may occur also in some patients. If you notice any other effects check with your doctor. |
|
Zoloft |
Mechanism of Action |
Inhibits neuronal uptake of serotonin. In this regard it is classified as a selective serotonin reuptake inhibitor (SSRI). |
Therapeutic Use |
Treatment of depression, obsessive-compulsive disorders and panic disorders. |
Absorption |
Fairly well absorbed. Peak plasma level reached 4-8 h after a single dose. |
Metabolism |
The principle initial pathway of Metabolism for sertraline is N-demethylation by P-450 system. |
Half-life |
26 hours |
Average Daily Dose (adult) |
100-150 mg |
Adverse Effects |
Headache, insomnia (disturbed sleep patterns), agitation, anxiety, dizziness, nausea. |
Drug Interaction |
Potential effects of coadministration of drugs highly metabolized by P-450 enzymes. |
Contraindication |
Concomitant use in patients taking monoamine oxidase inhibitors. |
|
Valium |
Mechanism of Action |
Same as for Lorazepam |
Therapeutic Use |
Same as for Lorazepam; and it can be given I.V. for status epilepticus. |
Absorption |
Well absorbed after oral administration. Peak plasma levels, 30-90 minutes. |
Metabolism |
Demethylated in the liver by P-450 enzymes and conjugated with glucuronic acid. |
Half-life |
20-60 hours |
Average Daily Dose (adult) |
4-40 mg |
Adverse Effects |
Same as Lorazepam |
Drug Interaction |
Same as Lorazepam, and with other drugs metabolized by P-450 enzymes in liver. |
Contraindication |
Same as Lorazepam Other side effects not listed above may occur also in some patients. If you notice any other effects check with your doctor. |
|
Xanax |
Mechanism of Action |
Same as Lorazepam, plus antidepressant action of unknown mechanism. |
Therapeutic Use |
Same as Lorazepam for anxiety. Can also be used in patients with panic disorder due to its antidepressant effects. May also be used in patients with depression. |
Absorption |
Well absorbed after oral administration. Peak blood levels reached in 1-2 hours. |
Metabolism |
Same as Lorazepam |
Half-life |
12 -15 hours. |
Average Daily Dose (adult) |
0.75-1.5 mg |
Adverse Effects |
Same as Lorazepam |
Drug Interaction |
Same as Lorazepam, and with other drugs metabolized by P-450 enzymes. |
Contraindication |
Same as Lorazepam Other side effects not listed above may occur also in some patients. If you notice any other effects check with your doctor |
These brief pharmaceutical summaries do not include all information important for patient use and should not be used as a substitute for professional medical advice. Consult the prescribing doctor and read package inserts before using these or any other medications or supplements.
CDER
U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES
Public Health Service
National Institutes of Health
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