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All about: Citalopram

Big Image Pronouncation: (sye-TAL-oh-pram)
Class: SSRI

Trade Names:
Celexa
- Tablets 10 mg
- Tablets 20 mg
- Tablets 40 mg
- Oral solution 10 mg per 5 mL

Mechanism of Action

Pharmacology

Inhibits the CNS neuronal uptake of serotonin, potentiating serotonergic activity.

Pharmacokinetics

Absorption

T max is about 4 h. About 80% bioavailable. Steady state reached in about 1 wk.

Distribution

Vd is about 12 L/kg. About 80% bound to plasma proteins.

Metabolism

Metabolized in the liver; CYP3A4 and CYP2C19 are the primary isozymes involved in N-demethylation of citalopram. Metabolites are demethylcitalopram (DCT), didemethylcitalopram (DDCT), citalopram-N-oxide, and deaminated propionic acid derivative; metabolites do not appear to contribute to antidepressant actions.

Elimination

About 10% is excreted in urine as citalopram. Systemic Cl is 330 mL/min (about 20% is due to renal Cl). The t ½ is about 35 h.

Special Populations

Renal Function Impairment

Oral Cl decreased by 17%.

Hepatic Function Impairment

Oral Cl decreased by 37% and t ½ doubled.

Elderly
Single dose

AUC increased 30% and t ½ increased 50%.

Multiple dose

AUC increased 23% and t ½ increased 30%.

Indications and Usage

Treatment of major depression as defined in DSM-III and DSM-III-R .

Unlabeled Uses

Treatment of panic disorder, obsessive-compulsive disorder, premenstrual dysphoria, posttraumatic stress disorder, generalized anxiety disorder.

Contraindications

Standard considerations; concomitant use of MAOIs or pimozide.

Dosage and Administration

Adults

PO Initiate with 20 mg once daily and titrate up to 40 mg/day; max, 60 mg/day.

Elderly

PO Initiate with 20 mg once daily; titrate up to 40 mg/day if needed.

Hepatic Function Impairment

PO Initiate with 20 mg once daily; titrate up to 40 mg/day if needed.

Maintenance

Periodically reevaluate long-term usefulness if used for extended periods.

General Advice

  • Administer dose once daily, in the morning or evening, without regard to meals. Administer with food if GI upset occurs.
  • Use dosing syringe, dosing spoon, or dosing cup to measure and administer prescribed dose of oral solution.

Storage/Stability

Store tablets and oral solution at controlled room temperature (59° to 86°F).

Drug Interactions

Beta-blockers (ie, carvedilol, metoprolol, propranolol)

Inhibition of beta-blocker's metabolism may occur, resulting in excessive beta blockade (eg, bradycardia). Coadministration of metoprolol with citalopram has increased plasma levels of metoprolol 2-fold.

Cimetidine

Serum levels of citalopram may be increased 40%.

CNS drugs

Use citalopram with caution in patient receiving CNS drugs.

Cyproheptadine

May decrease the pharmacologic effect of citalopram.

Ketoconazole

Ketoconazole plasma levels may be reduced slightly.

Lithium

Lithium may enhance the serotonergic effects of citalopram; use caution if coadministered.

MAOIs, pimozide

Concomitant use with citalopram is contraindicated.

Sumatriptan

Rare postmarketing reports of weakness, hyperreflexia, and incoordination following coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension, postural hypotension, tachycardia (at least 1%); QT prolongation, ventricular arrhythmia, torsades de pointes (postmarketing).

CNS

Somnolence (18%); insomnia (15%); tremor (8%); fatigue (5%); anorexia, anxiety (4%); agitation (3%); decreased libido, dizziness, yawning (2%); asthenia (1%); aggravated depression, amnesia, apathy, confusion, depression, increased appetite, impaired concentration, migraine, paresthesia, suicide attempts (at least 1%); akathisia, delirium, dyskinesia, grand mal convulsions, neuroleptic malignant syndrome, nystagmus (postmarketing).

Dermatologic

Increased sweating (11%); pruritus, rash (at least 1%), epidermal necrolysis, erythema multiforme (postmarketing).

EENT

Abnormal accommodation, taste perversion (at least 1%).

GI

Nausea (21%); dry mouth (20%); diarrhea (8%); dyspepsia (5%); vomiting (4%); abdominal pain (3%); flatulence, increased saliva (at least 1%); GI hemorrhage, pancreatitis (postmarketing).

Genitourinary

Ejaculation disorder (6%); dysmenorrhea, impotence (3%); amenorrhea, polyuria (at least 1%); acute renal failure. Priapism, prolactinemia, spontaneous abortion (postmarketing).

Hematologic-Lymphatic

Ecchymosis, hemolytic anemia, thrombocytopenia, thrombosis (postmarketing).

Hepatic

Hepatic necrosis (postmarketing).

Lab Tests

Decreased prothrombin (postmarketing).

Metabolic-Nutritional

Decreased weight (at least 1%).

Musculoskeletal

Arthralgia, myalgia (2%); myoclonus, rhabdomyolysis (postmarketing).

Respiratory

Upper respiratory tract infection, rhinitis (5%); sinusitis (3%); coughing (at least 1%).

Miscellaneous

Fever (2%); allergic reaction, anaphylaxis, angioedema, choreoathetosis, chest pain, serotonin syndrome, withdrawal syndrome (postmarketing).

Precautions

Warnings

Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term studies in children and adolescents with major depressive disorder and other psychiatric disorders. When considering the use of any antidepressant in a child or adolescent, balance this risk with clinical need. Closely observe children or adolescents for clinical worsening, suicidality, or unusual changes in behavior during the initial few months of therapy or at times of increases or decreases in dose. Advise families and caregivers of the need for close observation and communication with the prescriber.


Monitor

Monitor pediatric and adult patients for clinical worsening, suicidality, and unusual changes in behavior, especially during the first few months of therapy or at times of increases or decreases in dose. Evaluate children at least weekly with face-to-face contact with the patient or their family members or caregiver during the first 4 wk of therapy, then every other week for the next 4 wk, then at 12 wk, and as clinically indicated thereafter. The following symptoms may represent precursors to suicidality and should be reported to health care provider immediately if noted or suspected: aggressiveness, agitation, anxiety, hostility, hypomania, impulsivity, insomnia, irritability, mania, panic attacks, and psychomotor restlessness. Frequently assess patient for response to treatment. Periodically review therapy to determine if therapy needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated.


Pregnancy

Category C . Neonates exposed to citalopram late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding. Consider potential risks and benefits of treatment when treating women during the third trimester.

Lactation

Excreted in breast milk; may adversely affect infant.

Children

Safety and efficacy not established.

Elderly

May require lower dose; 20 mg/day is max recommended dose.

Renal Function

Use with caution in patients with severe renal impairment (Ccr less than 20 mL/min).

Hepatic Function

Use with caution; lower max dose is recommended.

Hazardous Tasks

May impair judgment, thinking, or motor skills.

Photosensitivity

Has been rarely reported.

Abnormal bleeding

Bleeding episodes have occurred in patients treated with psychotropic drugs that interfere with serotonin reuptake.

Activation of mania/hypomania

Has been reported. Use cautiously in patients with history of mania/hypomania.

Concomitant illness

Use with caution in patients with diseases or conditions that could affect hemodynamic responses or metabolism. Consider using lower or less frequent dosing.

Discontinuation of treatment

Withdrawal symptoms have been reported following rapid discontinuation of therapy. If treatment is to be discontinued or the dose reduced, gradually taper the dose and monitor patient for withdrawal symptoms (eg, abnormal skin sensations, agitation, anxiety, confusion, dizziness, dysphoric mood, emotional lability, headaches, hypomania, insomnia, irritability, lethargy). If significant withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.

Hyponatremia

Hyponatremia and/or SIADH may occur. Use with caution in patients who are elderly, volume-depleted, or taking diuretics.

Screening for bipolar disorder

A major depressive episode may be the initial presentation of bipolar disorder and treating such an episode with an antidepressant alone may increase the likelihood of precipitating a mixed/manic episode in patients at risk for bipolar disorder. Screen patients with depression for risk of bipolar disorder prior to initiating therapy with an antidepressant.

Seizures

May occur; use with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold. Discontinue use if seizures occur.

Suicide

Suicidal ideation is inherent in depression and may persist until significant remission occurs. Closely supervise high-risk patients during initial drug therapy. Prescribe smallest quantity of medication consistent with good patient management in order to reduce risk of overdose.

Overdosage

Symptoms

Amnesia, coma, confusion, convulsions, cyanosis, dizziness, ECG changes (including QT prolongation, nodal rhythm, ventricular arrhythmia, torsades de pointes), hyperventilation, nausea, rhabdomyolysis, sinus tachycardia, somnolence, sweating, tremor, vomiting.

Patient Information

  • Advise patient or caregiver to read the Medication Guide before starting therapy and each time the medication is refilled, especially if patient is a child or adolescent.
  • Advise patient that dose will usually be started low and then increased until max benefit is obtained.
  • Instruct patient to take prescribed dose once daily, in the morning or evening without regard to meals, but to take with food if stomach upset occurs.
  • Advise patient or caregiver using oral solution to measure and administer prescribed dose using dosing syringe, dosing spoon, or dosing cup.
  • Advise patient that if a dose is missed to take it as soon as possible and then return to the normal schedule. However, if it is almost time for the next dose, to skip the missed dose and take the next dose at the regularly scheduled time. Instruct patient that if a dose is skipped not to double the dose to catch up.
  • Instruct patient not to change the dose or stop taking unless advised by health care provider.
  • Advise patient or caregiver that it may take between 1 and 4 wk of therapy before improvement is noted and not to stop taking the medication when they feel better.
  • Caution patient not to take aspirin or aspirin-containing products, NSAIDs, ginkgo biloba, or any other medication or herbal product that can affect coagulation unless advised by health care provider, because of increased risk of serious bleeding.
  • Instruct patient to contact health care provider if symptoms do not appear to be getting better, worsen, or if bothersome side effects (eg, excessive drowsiness, diarrhea, tremors, nausea, diarrhea, nervousness, changes in sexual function) occur.
  • Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
  • Advise patient being treated for depression, and family or caregiver of patient, to be alert for abnormal changes in mood or thinking and to immediately report any of the following to health care provider: change in personality; change in mood; anxiety; agitation; panic attacks; insomnia; irritability; hostility or aggressiveness; impulsivity; akathisia (psychomotor restlessness); or suicidal thoughts or behavior. Advise families and caregivers of patients to observe for emergence on a day-to-day basis, because changes may be abrupt.
  • Instruct patient or caregiver to immediately report rash, hives, or itching to health care provider.
  • Advise patient that if medication needs to be discontinued it will be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
  • Advise patient that medication may increase sensitivity to sunlight. Caution patient to avoid unnecessary exposure to UV light (sunlight, tanning booths) and to use sunscreen and wear protective clothing when exposed to UV light.
  • Instruct patient to avoid alcoholic beverages and sedatives or depressants (eg, diazepam) while taking medication.
  • Advise patient that drug may impair judgment, thinking, motor skills, or cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.

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