Q

Q



quazepam


(kway’-ze-pam)


image Brand Name(s): Doral


Chemical Class: Benzodiazepine


DEA Class: Schedule IV


image Clinical Pharmacology:



Mechanism of Action: A BZ-1 receptor selective benzodiazepine with sedative properties. Therapeutic Effect: Produces sedative effect from its central nervous system (CNS) depressant action.

Pharmacokinetics:



image

Rapidly absorbed from gastrointestinal (GI) tract. Food increases absorption. Protein binding: 95%. Extensively metabolized in liver. Excreted in urine and feces. Unknown if removed by hemodialysis. Half-life: 25-41 hr.


image Available Forms:


• Tablets: 7.5 mg, 15 mg.

image Indications and Dosages:


Insomnia: PO Initially, 7.5-15 mg at bedtime. Adjust dose depending on initial response.

image Contraindications: Sleep apnea, hypersensitivity to quazepam or any component of the formulation




image Side Effects



Frequent

Muscular incoordination (ataxia), light-headedness, transient mild drowsiness, slurred speech

Occasional

Confusion, depression, blurred vision, constipation, diarrhea, dry mouth, headache, nausea

Rare

Behavioral problems such as anger, impaired memory; paradoxical reactions such as insomnia, nervousness, or irritability


image Serious Reactions



• Abrupt or too-rapid withdrawal may result in pronounced restlessness, irritability, insomnia, hand tremors, abdominal and muscle cramps, sweating, vomiting, and seizures.

• Overdosage results in somnolence, confusion, diminished reflexes, and coma.

• Blood dyscrasias have been reported rarely.


image Patient/Family Education



• Avoid alcohol and other CNS depressants

• Do not discontinue abruptly after prolonged therapy

• May cause daytime sedation, use caution while driving or performing other tasks requiring alertness

• May be habit forming

• Stop smoking


image Monitoring Parameters



• Hepatic and renal function

• Therapeutic response

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls

Other: None

image Use with caution in older patients with: Concurrent treatment with potent CYP 3A4 inhibitors leads to increased plasma concentrations of quazepam; COPD; untreated sleep apnea



image U.S. Regulatory Considerations



image FDA Black Box

image OBRA regulated in U.S. Long Term Care

image Other Uses in Geriatric Patient: Anxiety symptoms and related disorders; dementia-related behavioral problems


image Side Effects:


Of particular importance in the geriatric patient: Sedation


image Geriatric Considerations – Summary: Benzodiazepines are effective anxiolytic agents, and hypnotics. These drugs should be reserved for short-term use. SSRIs are preferred for long-term management of anxiety disorders in older adults, and sedating antidepressants (e.g., trazodone) or eszopiclone are preferred for long-term management of sleep problems. Long-acting benzodiazepines, including flurazepam, chlordiazepoxide, clorazepate, diazepam, clonazepam, and quazepam should generally be avoided in older adults as these agents have been associated with oversedation. On the other hand, short-acting benzodiazepines (e.g., triazolam) have been as- sociated with a higher risk of withdrawal symptoms. When initiating therapy, benzodiazepines should be titrated carefully to avoid oversedation. In addition, many of the drugs in this class have been associated with severe withdrawal symptoms (e.g., anxiety and/or agitation, seizures) when discontinued abruptly.



Reference



1 Leipzig RM, Cumming RG, Tinetti ME. Drugs and falls in older people: a systematic review and meta-analysis: I. Psychotropic drugs. J Am Geriatr Soc. 1999;47:30-39.


2 Shorr RI, Robin DW. Rational use of benzodiazepines in the elderly. Drugs Aging. 1994;4:9-20.


3 Shader RI, Greenblatt DJ. Use of benzodiazepines in anxiety disorders. N Engl J Med. 1993;328:1398-1405.



quetiapine fumarate


(kwe-tye’-a-peen fyoo’-muh-rate)


image Brand Name(s): Seroquel


Chemical Class: Dibenzothiazepine derivative


image Clinical Pharmacology:



Mechanism of Action: A dibenzothiazepine derivative that antagonizes dopamine, serotonin, histamine, and alpha1-adrenergic receptors. Therapeutic Effect: Diminishes manifestations of psychotic disorders. Produces moderate sedation, few extrapyramidal effects, and no anticholinergic effects.

Pharmacokinetics: Well absorbed after PO administration. Protein binding: 83%. Widely distributed in tissues; CNS concentration exceeds plasma concentration. Undergoes extensive first-pass metabolism in the liver. Primarily excreted in urine. Half-life: 6 hr.

image Available Forms:


• Tablets: 25 mg, 100 mg, 200 mg, 300 mg.

image Indications and Dosages:


To manage manifestations of psychotic disorders: PO Initially, 25 mg twice a day, then 25-50 mg 2-3 times a day on the second and third days, up to 300-400 mg/day in divided doses 2-3 times a day by the fourth day. Further adjustments of 25-50 mg twice a day may be made at intervals of 2 days or longer. Maintenance: 300-800 mg/day (adults); 50-200 mg/day (elderly).

Mania in bipolar disorder: PO Initially, 50 mg twice a day for 1 day. May increase in increments of 100 mg/day to 200 mg twice a day on day 4. May increase in increments of 200 mg/day to 800 mg/day on day 6. Range: 400-800 mg/day.

Dosage in hepatic impairment, elderly or debilitated patients, and those predisposed to hypotensive reactions: These patients should receive a lower initial dose and lower dosage increases.

image Unlabeled Uses: Autism


image Contraindications: None known.




image Side Effects



Frequent (19%-10%)

Headache, somnolence, dizziness

Occasional (9%-3%)

Constipation, orthostatic hypotension, tachycardia, dry mouth, dyspepsia, rash, asthenia, abdominal pain, rhinitis

Rare (2%)

Back pain, fever, weight gain


image Serious Reactions



• Overdose may produce heart block, hypotension, hypokalemia, and tachycardia.


Special Considerations



• Limited clinical experience, but similar to clozapine and risperidone; may be effective for negative symptoms of schizophrenia; so far no agranulocytosis reported with quetiapine


image Patient/Family Education



• Avoid alcohol

• Take quetiapine as ordered; do not abruptly discontinue the drug or increase the dosage

• Drowsiness generally subsides during continued therapy

• Avoid tasks that require mental alertness or motor skills until response to the drug has been established

• Change positions slowly to reduce the hypotensive effect of quetiapine

• Drink lots of fluids, especially during physical activity


image Monitoring Parameters



• Blood pressure for hypotension and pulse rate for tachycardia, especially if the drug dosage has been increased rapidly

• Pattern of daily bowel activity and stool consistency

• Assess for evidence of a therapeutic response, such as improvement in self-care, increased interest in surroundings and ability to concentrate, and relaxed facial expression

• Closely supervise suicidal patients during early therapy; as depression lessens, the patient’s energy level improves, which increases the suicide potential

image Geriatric side effects at a glance:



image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls

Other: Weight gain, glucose intolerance, diabetes, orthostatic hypotension, extrapyramidal symptoms


image Use with caution in older patients with: Diabetes, glucose intolerance, cardiovascular disease



image U.S. Regulatory Considerations



image FDA Black Box

There is an increased risk of death in older patients with dementia. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. This drug is not approved for treatment of patients with dementia-related psychosis.


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Jun 8, 2016 | Posted by in GERIATRICS | Comments Off on Q

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