Ariprazo

Details About Generic Salt ::  Ariprazo

Main Medicine Class:: Antipsychotic agent   

(A-rih-PIP-ray-zole)
Abilify
Tablets: 10 mg
Tablets: 15 mg
Tablets: 20 mg
Tablets: 30 mg
Class: Antipsychotic agent

 

Drugs Class ::

 Action Partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and antagonist at serotonin 5-HT2A receptor.

Absorption: Well absorbed; steady state is attained within 14 days. Tmax is 3 to 5 hr and bioavailability is 87%.

Distribution: More than 99% is protein bound, primarily to albumin. Vd is 404 L or 4.9 L/kg.

Metabolism: Hepatic metabolism (dehydrogenation, hydroxylation, and N-dealkylation) involives CYP2D6 and CYP 3A4. Major metabolite is dehydro-aripiprazole (active).

Elimination: Approximately 25% excreted in urine (less than 1% unchanged) and 55% in feces (approximately 18% as unchanged drug). The elimination half-life is 75 hr (aripiprazole) and 94 hr (dehydro-aripiprazole).

Special Populations: Hepatic function impairment: AUC increased 31% in mild hepatic impairment, increased 8% in moderate impairment, and decreased 20% in severe impairment. No dosage adjustment required. Renal function impairment: In severe renal impairment (Ccr less than 30 mL/min), Cmax increased 36% (parent drug) and 53% (metabolite), but AUC was 15% lower for aripiprazole and 7% higher for metabolite. No dosage adjustment needed. Elderly: Clearance was 20% lower. No dosage adjustment required. Gender: Cmax and UAC are 30% to 40% higher in women than in men. No dosage adjustement required.

Indications for Drugs ::

 Indications Treatment of schizophrenia.

Drug Dose ::

 Route/Dosage

Usual Dose

Adults: PO Start with 10 or 15 mg/day on a once-daily schedule. The effective dose range is 10 to 30 mg/day. Do not increase dosage before 2 wk.

Concurrent Use of CYP3A4 (eg, ketoconazole) or CYP2D6 Inhibitors (eg, fluoxetine, quinidine)

Adults: PO Reduce the usual dose of aripiprazole 50%. Increase the dose when the CYP3A4 inhibitor is discontinued.

Concurrent Use of CYP3A4 Inducers (eg, carbamazepine)

Adults: PO Double the usual dose of aripiprazole (to 20 to 30 mg). Additional increases should be based on clinical evaluation. Decrease the dose (to 10 to 15 mg) when the CYP3A4 inducer is discontinued.

Maintenance No evidence is available from controlled trials; however, it is generally agreed that treatment for acute schizophrenia should be continued for up to 6 mo or more.

Contraindication ::

 Contraindications Standard considerations.

Drug Precautions ::

 Precautions

Pregnancy: Category C. Lactation: Undetermined. Children: Safety and efficacy not established. Aspiration pneumonia: Antipsychotics have been associated with esophageal dysmotility and aspiration; use with caution in patients at risk for aspiration pneumonia. Cognitive and motor skills: Cognitive and motor skills may be impaired; caution patients about operating hazardous machinery or driving until they are reasonably certain that therapy does not affect them adversely. Neuroleptic malignant syndrome: Neuroleptic malignant syndrome has occurred with antipsychotics and is potentially fatal. Signs and symptoms are hyperpyrexia, muscle rigidity, altered mental status, irregular pulse, irregular BP, tachycardia, and diaphoresis. Orthostatic hypotension: Orthostatic hypotension may occur. Psychosis associated with Alzheimer disease or dementia: Use with caution. Seizures: Seizures may occur; use with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold. Suicide: Closely supervise high-risk patients; do not give excessive quantities. Tardive dyskinesia: A potentially irreversible syndrome of involuntary body and facial movements may occur. Temperature regulation: Antipsychotics can disrupt the body’s ability to reduce core temperature.

PATIENT CARE CONSIDERATIONS


Drug Side Effects ::

 Adverse Reactions

CARDIOVASCULAR: Hypertension; tachycardia; hypotension; bradycardia. CNS: Headache; anxiety; insomnia; lightheadedness; somnolence; akathisia; tremor; extrapyramidal symptoms; depression; nervousness; increased salivation; hostility; suicidal thought; manic reaction; abnormal gait; confusion; cogwheel rigidity. DERMATOLOGIC: Rash; dry skin; pruritus; sweating; skin ulcer. EENT: Rhinitis; blurred vision; conjunctivitis; ear pain. GI: Nausea; vomiting; constipation; anorexia; nausea. GU: Urinary incontinence. HEMATOLOGIC: Ecchymosis; anemia. METABOLIC: Weight gain; weight loss, increased creatine phosphokinase. RESPIRATORY: Coughing; dyspnea; pneumonia. OTHER: Asthenia; fever; flu syndrome; peripheral edema; chest pain; neck pain; neck rigidity; hypothyroidism; muscle cramps.

Drug Mode of Action ::  

 Action Partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and antagonist at serotonin 5-HT2A receptor.

Absorption: Well absorbed; steady state is attained within 14 days. Tmax is 3 to 5 hr and bioavailability is 87%.

Distribution: More than 99% is protein bound, primarily to albumin. Vd is 404 L or 4.9 L/kg.

Metabolism: Hepatic metabolism (dehydrogenation, hydroxylation, and N-dealkylation) involives CYP2D6 and CYP 3A4. Major metabolite is dehydro-aripiprazole (active).

Elimination: Approximately 25% excreted in urine (less than 1% unchanged) and 55% in feces (approximately 18% as unchanged drug). The elimination half-life is 75 hr (aripiprazole) and 94 hr (dehydro-aripiprazole).

Special Populations: Hepatic function impairment: AUC increased 31% in mild hepatic impairment, increased 8% in moderate impairment, and decreased 20% in severe impairment. No dosage adjustment required. Renal function impairment: In severe renal impairment (Ccr less than 30 mL/min), Cmax increased 36% (parent drug) and 53% (metabolite), but AUC was 15% lower for aripiprazole and 7% higher for metabolite. No dosage adjustment needed. Elderly: Clearance was 20% lower. No dosage adjustment required. Gender: Cmax and UAC are 30% to 40% higher in women than in men. No dosage adjustement required.

Drug Interactions ::

 Interactions

Alcohol: Avoid while using aripiprazole. CYP2D6 inhibitors (eg, fluoxetine, paroxetine, quinidine), CYP3A4 inhibitors (eg, ketoconazole): May elevate aripiprazole plasma levels, increasing the adverse effects. CYP2D6 inducers (eg, carbamazepine): May reduce aripiprazole plasma levels, decreasing the therapeutic effect.

Drug Assesment ::

 Assessment/Interventions

  • Obtain patient history, including drug history and any known allergies. Note history of CV disease, cerebrovascular disease, cardiac arrhythmias, previous episodes of neuroleptic malignant syndrome, seizures, or Alzheimer disease.
  • Note concurrent use of CYP2D6 inhibitor, CYP3A4 inhibitor or inducer, or antihypertensive therapy.
  • Monitor cardiac patients during initiation of drug for orthostatic hypotension; notify health care provider if noted.
  • Take safety precautions if orthostatic hypotension occurs.
  • Inform health care provider immediately if hyperpyrexia, muscle rigidity, altered mental status, irregular pulse and BP, tachycardia, and diaphoresis develop.
  • Notify health care provider if any of the following develops: hypotension; tachycardia; excessive drowsiness; nausea; vomiting; constipation; indigestion.
  • Assess baseline neurologic status and during treatment observe for involuntary body and facial movements, drowsiness, agitation, anxiety, aggressive reaction, or seizure activity.
  • Monitor patient for suicidal tendencies often associated with schizophrenia.
  • Assess medication compliance.
OVERDOSAGE: SIGNS & SYMPTOMS
  Somnolence, vomiting

Drug Storage/Management ::

 Administration/Storage

  • Administer prescribed dose once daily without regard to meals.
  • Administer with food if GI upset occurs.
  • Store at controlled room temperature (59° to 86° F).

Drug Notes ::

 Patient/Family Education

  • Explain name, dose, action, and potential side effects of drug.
  • Instruct patient to take prescribed dose once daily without regard to meals but to take with food if GI upset occurs.
  • Instruct patient not to stop taking aripiprazole feeling better.
  • Tell patient to immediately report high fever, muscle rigidity, altered mental status, irregular pulse, sweating, seizures, or rash to health care provider.
  • Advise patient to avoid strenuous activity during periods of high temperature or humidity.
  • Instruct patient to avoid alcoholic beverages while taking aripiprazole.
  • Instruct patients to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension. Advise patient to report dizziness with position changes to health care provider. Caution patient that hot tubs and hot showers or baths may make dizziness worse.
  • Advise patient taking antithypertensives to monitor BP at regular intervals.
  • Advise patient that drug may impair judgment, thinking, or motor skills or cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
  • Instruct women to notify health care provider if pregnant, planning to become pregnant, or breastfeeding.
  • Advise patient to notify health care provider of the following symptoms: excessive drowsiness, increased agitation or anxiety, involuntary body or facial movements, rapid pulse, nausea, vomiting, constipation.
  • Instruct patient to not take any prescription or OTC medications or dietary supplements unless advised by health care provider.
  • Advise patient that follow-up visits will be required to monitor therapy and to keep appointments.

Disclaimer ::

The Information available on this site is for only Informational Purpose , before any use of this information please consult your Doctor .Price of the drugs indicated above may not match to real price due to many possible reasons may , including local taxes etc.. These are only approximate indicative prices of the drug.

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