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Antianxiety Drugs

Definition, Purpose, Description, Recommended dosage, Precautions, Side effects, Interactions

Antianxiety drugs are medicines that calm and relax people with excessive anxiety, nervousness, or tension, or for short term control of social phobia disorder or specific phobia disorder.

Purpose

Antianxiety agents, or anxiolytics, may be used to treat mild transient bouts of anxiety as well as more pronounced episodes of social phobia and specific phobia. Clinically significant anxiety is marked by several symptoms. The patient experiences marked or persistent fear of one or more social or performance situations in which he or she is exposed to unfamiliar people or possible scrutiny by others, and may react in a humiliating or embarrassing way. The exposure to the feared situation produces an anxiety attack. Fear of these episodes of anxiety leads to avoidance behavior, which impairs normal social functioning, including working or attending classes. The patient is aware that these fears are unjustified.

Description

In psychiatric practice, treatment of anxiety has largely turned from traditional antianxiety agents, anxiolytics, to antidepressant therapies. In current use, the benzodiazepines, the best known class of anxiolytics, have been largely supplanted by serotonin-specific reup-take inhibitors (SSRIs, citalopram, fluoxetine, fluvoxamine and others) which have a milder side effect profile and less risk of dependency. However, traditional anxiolytics remain useful for patients who need a rapid onset of action, or whose frequency of exposure to anxiety provoking stimuli is low enough to eliminate the need for continued treatment. While SSRIs may require three to five weeks to show any effects, and must be taken continuously, benzodiazepines may produce a response within 30 minutes, and may be dosed on an as-needed basis.

The intermediate action benzodiazepines, alprazolam (Xanax), and lorazepam (Ativan) are the appropriate choice for treatment of mild anxiety and social phobia. Diazepam (Valium) is still widely used for anxiety, but its active metabolite, desmethyldiazepam, which has a long half-life, may make this a poorer choice than other drugs in its class. Note that there is considerable variation between individuals in metabolism of benzodiazepines, so patient response may not be predictable. As a class, benzodiazepines are used not only as anxiolytics, but also as sedatives, muscle relaxants, and in treatment of epilepsy and alcoholism. The distinctions between these uses are largely determined by onset and duration of action, and route of administration.

Buspirone (BuSpar), which is not chemically related to other classes of central nervous system drugs, is also a traditional anxiolytic, although it is now considered either a third line or adjunctive agent for use after trials of SSRIs and benzodiazepines. It is appropriate for use in patients who have either failed trials of other treatments, or who should not receive benzodiazepines because of a history of substance abuse problems. Buspirone, in common with antidepressants, requires a two to three week period before there is clinical evidence of improvement, and must be continuously dosed to maintain its effects.

Antianxiety Drugs

Antianxiety Drugs
Brand Name (Generic Name) Possible Common Side Effects Include:
Atarax (hydroxyzine hydrochloride) Drowsiness, dry mouth
Ativan (lorazepam) Dizziness, excessive calm, weakness
BuSpar, Buspirone (buspirone hydrochloride) Dry mouth, dizziness, headache, fatigue, nausea
Centrax (pazepam) Decreased coordination, dizziness, drowsiness, fatigue, weakness
Librium, Libritabs (chlordiazepoxide) Constipation, drowsiness, nausea, swelling
Miltown, Equanil (meprobamate) Diarrhea, bruising, fever, headache, nausea, rash, slurred speech
Serax (oxazepam) Dizziness, fainting, headache, liver problems, decreased coordination, nausea, swelling, vertigo
Stelazine (trifluoperazine hydrochloride) Abnormal glucose in urine, allergic reactions, blurred vision, constipation, eye spasms, fluid retention and swelling
Tranxene, Tranxene-SD (clorazepate dipotassium) Drowsiness
Valium (diazepam) Decreased coordination, drowsiness, light-headedness

Benzodiazepines are controlled drugs under federal law. Buspirone is not a controlled substance and has no established abuse potential.

Recommended dosage

Benzodiazepines should be administered 30 to 60 minutes before exposure to the anticipated stress. Dosage should be individualized to minimize sedation. The normal dose of alprazolam is 0.25–0.5 mg. The usual dose of lorazepam is 2–3 mg. Doses may be repeated if necessary.

Buspirone is initially dosed at 5 mg t.i.d. (3 times a day.) Increase the dosage 5 mg/day, at intervals of two to three days, as needed. Do not exceed 60 mg/day. Two to three weeks may be required before a satisfactory response is seen.

Precautions

Benzodiazepines should not be used in patients with psychosis, acute narrow angle glaucoma, or liver disease. The drugs can act as respiratory depressants and should be avoided in patients with respiratory conditions. Benzodiazepines are potentially addictive and should not be administered to patients with substance abuse disorders. Because benzodiazepines are sedative, they should be avoided in patients who must remain alert. Their use for periods over four months has not been documented. These drugs should not be used during the second and third trimester of pregnancy, although use during the first trimester appears to be safe. They should not be taken while breastfeeding. Consult specialized references for use in children.

Buspirone is metabolized by the liver and excreted by the kidney, and should be used with care in patients with hepatic or renal disease. The drug is classified as schedule B during pregnancy, but should not be taken during breastfeeding. Its use in children under the age of 18 years has not been studied.

Side effects

The most common side effects of benzodiazepines are secondary to their CNS effects and include sedation and sleepiness; depression; lethargy; apathy; fatigue; hypoactivity; lightheadedness; memory impairment; disorientation; anterograde amnesia; restlessness; confusion; crying or sobbing; delirium; headache; slurred speech; aphonia; dysarthria; stupor; seizures; coma; syncope; rigidity; tremor; dystonia; vertigo; dizziness; euphoria; nervousness; irritability; difficulty in concentration; agitation; inability to perform complex mental functions; akathisia; hemiparesis; hypotonia; unsteadiness; ataxia; incoordination; weakness; vivid dreams; psychomotor retardation; "glassy-eyed" appearance; extrapyramidal symptoms; paradoxical reactions. Other reactions include changes in heart rate and blood pressure, changes in bowel function, severe skin rash and changes in genitourinary function. Other adverse effects have been reported.

Buspirone has a low incidence of side effects. Dizziness and drowsiness are the most commonly reported adverse effects. Other CNS effects include dream disturbances; depersonalization, dysphoria, noise intolerance, euphoria, akathisia, fearfulness, loss of interest, disassociative reaction, hallucinations, suicidal ideation, seizures; feelings of claustrophobia, cold intolerance, stupor and slurred speech, psychosis. Rarely, heart problems, including congestive heart failure and myocardial infarction, have been reported. Other adverse effects have been reported.

Interactions

The metabolism of alprazolam may be increased by: cimetidine, oral contraceptives, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, propoxyphene, propranolol and valproic acid. The absorption of all benzodiazepines is inhibited by concomitant use of antacids. Benzodiazepines may increase blood devels of digoxin, and reduce the efficacy of levodopa. Other drug interactions have been reported.

Buspirone levels will be increased by concomitant use of erythromycin, itraconazole, and nefazadone. Doses should be adjusted based on clinical response. Use of buspirone at the same time as mono-amine oxidase inhibitors (MAOIs, phenelzine, tranycypromine) may cause severe blood pressure elevations. Use of buspirone with MAOIs should be avoided.

Samuel Uretsky, PharmD

KEY TERMS


Anxiety—Worry or tension in response to real or imagined stress, danger, or dreaded situations. Physical reactions, such as fast pulse, sweating, trembling, fatigue, and weakness may accompany anxiety.

Epilepsy—A brain disorder with symptoms that include seizures.

Panic disorder—An disorder in which people have sudden and intense attacks of anxiety in certain situations. Symptoms such as shortness of breath, sweating, dizziness, chest pain, and extreme fear often accompany the attacks.

Phobia—An intense, abnormal, or illogical fear of something specific, such as heights or open spaces.

Pregnancy category B—Animal studies indicate no fetal risk, but no human studies; or adverse effects in animals, but not in well-controlled human studies.

Pregnancy category C—No adequate human or animal studies; or adverse fetal effects in animal studies, but no available human data.

Seizure—A sudden attack, spasm, or convulsion.

Additional topics

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