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Thursday, February 10, 2011

sildenafil citrate

Posted by Sampil 2:21 AM, under | 7 comments

sildenafil citrate
(sill den' ah fill)
Revatio, Viagra

Pregnancy Category B

Drug class
Impotence drug
Phosphodiesterase inhibitor

Therapeutic actions
Selectively inhibits cGMP-specific phosphodiesterase type 5. The mechanism of penile erection involves the release of nitric oxide into the corpus cavernosum of the penis during sexual stimulation. Nitrous oxide activates cGMP, which causes smooth muscle relaxation, allowing the flow of blood into the corpus cavernosum.Sildenafil prevents the breakdown of cGMP by phosphodiesterase, leading to increased cGMP levels and prolonged smooth muscle relaxation, promoting the flow of blood into the corpus cavernosum, and decreasing pressure in the pulmonary bed.

Indication
·        Treatment of erectile dysfunction in the presence of sexual stimulation
·        Treatment of pulmonary arterial hypertension to improve exercise ability

Contraindications and cautions
·        Contraindicated with allergy to any component of the tablet, contraindicated for women or children; concomitant use of nitrates.
·        Use cautiously with hepatic or renal dysfunction; with anatomical deformation of the penis; with known cardiac disease (effects of sexual activity need to be evaluated).

Available forms
Tablets—20 mg (Revatio); 25, 50, 100 mg

Dosages
ADULTS
·        Erectile dysfunction: 50 mg PO taken 1 hr before anticipated sexual activity; range 25–100 mg PO. May be taken 30 min–4 hr before sexual activity. Limit use to once per day.
·        Pulmonary arterial hypertension: 20 mg PO tid, at least 4–6 hr apart and without regard to food.
PEDIATRIC PATIENTS
Not intended for use in children.
GERIATRIC PATIENTS
For patients > 65 yr, start dose at 25 mg PO.
PATIENTS WITH RENAL OR HEPATIC IMPAIRMENT
Patients with hepatic impairment or creatinine clearance < 30 mL/min may have increased serum levels; start dose at 25 mg PO.

Pharmacokinetics
Route
Onset
Peak
Oral
Rapid
30–120 min

Metabolism: Hepatic; T1/2: 4 hr
Distribution: Not intended for use in women, no clear studies on crossing the placenta or entering breast milk
Excretion: Feces and urine

Adverse effects
·        CNS: Headache, abnormal vision, dizziness, nasal congestion, ischemic optic neuropathy
·        CV: Flushing
·        GI: Dyspepsia, diarrhea
·        Other: UTI, rash

Interactions
·        WARNING: Possible severe hypotension and serious cardiac events if combined with nitrates or alpha adrenergic blockers; this combination must be avoided
·        Possible increased sildenafil levels and effects if taken with cimetidineamlodipine, erythromycin, protease inhibitors; monitor patient and reduce dosage as needed
·        Decreased rate of absorption and onset of action if taken with a high-fat meal
·        Decreased metabolism and risk of toxic effects if combined with grapefruit juice; avoid this combination
·        Concomitant use may result in decrease in BP, orthostatic hypertension

Nursing considerations
Assessment
·        History: Allergy to any component of the tablet; hepatic or renal dysfunction; with anatomical deformation of the penis, known cardiac disease; concomitant use of nitrates
·        Physical: Orientation, affect; skin color, lesions; P, BP, ECG, LFTs, renal function tests

Interventions
·        Ensure diagnosis of pulmonary arterial hypertension (Revatio)
·        Ensure diagnosis of erectile dysfunction and determine underlying causes and other appropriate treatment.
·        Advise patient that drug does not work in the absence of sexual stimulation. Limit use to once per day.
·        Remind patient that drug does not protect against sexually transmitted diseases and appropriate measures should be taken.
·        WARNING: Advise patient to never take this drug with nitrates; serious and even fatal complications can occur.
·        WARNING: Advise patients receiving HIV medications that there is an increased risk of sidenafil-associated adverse drug reactions, including hypotension, visual changes, and priapism. Do not exceed 25 mg of sildenafil in 48 hr.
·        WARNING: Advise patients not to take this drug within 4 hr of administration of alpha blockers.

Teaching points
·        Take this drug 30 minutes to 4 hours before anticipated sexual activity. The usual timing is 1 hour. The drug will have no effect in the absence of sexual stimulation for erectile dysfunction.
·        If taking this drug for pulmonary arterial hypertension, take three times a day; make sure the doses are 4-6 hours apart.
·        Onset of drug effects will be slowed if taken with a high-fat meal; plan accordingly. Avoid drinking grapefruit juice if using this drug.
·        This drug will not protect you from sexually transmitted diseases; use appropriate precautions.
·        Stop the drug and call your health care provider immediately if you experience sudden loss of vision.
·        Do not take this drug if you are taking any nitrates; serious side effects and even death can occur.
·        You may experience these side effects: Headache, dizziness, rash, flushing.
·        Report difficult or painful urination, rash, dizziness, palpitations, loss of vision.

Adverse effects in Italic are most common; those in Bold are life-threatening.

7 comments:


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