ta-DA-la-fil

Therapeutic Classification:erectile dysfunction agents, vasodilators

Pharmacologic Classification: phosphodiesterase type 5 inhibitors

• Cialis: Treatment of:
  • Erectile dysfunction (ED),
  • Benign prostatic hyperplasia (BPH).
• Adcirca, Alyq, and Tadliq: Pulmonary arterial hypertension (PAH).

• Increases cyclic guanosine monophosphate (cGMP) levels by inhibiting phosphodiesterase type 5 an enzyme responsible for the breakdown of cGMP. cGMP produces smooth muscle relaxation of the corpus cavernosum, which in turn promotes increased blood flow and subsequent erection. cGMP also leads to vasodilation of the pulmonary vasculature.

• Cialis: Enhanced blood flow to the corpus cavernosum and erection sufficient to allow sexual intercourse.
• Improved signs and symptoms of BPH.
• Adcirca, Alyq, and Tadliq: Improved exercise tolerance in PAH.

Absorption: Well absorbed following oral administration.

Distribution: Extensive tissue distribution; penetrates semen.

Protein Binding: 94%.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP3A4 isoenzyme system; metabolites are excreted in feces (61%) and urine (36%).

Half-life: 17.5 hr.

(vasodilation, improved erectile function)

Contraindicated in:

• Hypersensitivity
• Concurrent use of nitrates or riociguat
• Unstable angina, recent history of stroke, life-threatening heart failure within 6 mo, uncontrolled hypertension, arrhythmias, stroke within 6 mo or MI within 90 days
• Any other cardiovascular pathology precluding sexual activity
• Known hereditary degenerative retinal disorders
• Severe hepatic impairment
• Severe renal impairment (Adcirca, Alyq, and Tadliq)
• Severe renal impairment (CCr <30 mL/min) (Cialis once-daily dosing)
• Pedi: Children or newborns.

Use Cautiously in:

• Left ventricular outflow obstruction
• Penile deformity
• Renal impairment
• Underlying conditions predisposing to priapism including sickle cell anemia, multiple myeloma, or leukemia
• Bleeding disorders or active peptic ulcer disease
• History of sudden severe vision loss or nonarteritic ischemic optic neuropathy; may ↑ risk of recurrence
• Low cup-to-disk ratio, age >50 yr, diabetes, hypertension, coronary artery disease, hyperlipidemia, or smoking (↑ risk of nonarteritic ischemic optic neuropathy)
• Geri: ↑risk of diarrhea in older adults.

CV: hypotension, peripheral edema.

Derm: flushing.

EENT: hearing loss, nasal congestion, vision loss.

GI: diarrhea, dyspepsia.

GU: ↓fertility, priapism.

MS: back pain, limb pain, myalgia.

Neuro: headache.

Drug-Drug:

• Concurrent use of nitrates may cause serious, life-threatening hypotension and is contraindicated.
• Concurrent use of riociguat may result in severe hypotension; concurrent use contraindicated.
• ↑risk of hypotension with alpha-adrenergic blockers and acute ingestion of alcohol; discontinue alpha-adrenergic blocker therapy 1 day before starting Cialis for BPH.
• Strong CYP3A4 inhibitors, including ritonavir, ketoconazole, anditraconazole, may ↑ levels and the risk of toxicity (dose adjustments recommended with Cialis; avoid concurrent use with Adcirca, Alyq, and Tadliq).
• CYP3A4 inducers may ↓ levels and its effectiveness; avoid concurrent use with Adcirca, Alyq, or Tadliq.

Cialis (for ED)

• PO (Adults): 10 mg prior to sexual activity (range 5–20 mg; not to exceed one dose/24 hr) or 2.5 mg once daily (max: 5 mg/day); Concurrent use of strong CYP3A4 inhibitors: single dose should not exceed 10 mg in any 72-hr period; for once-daily dose regimen, should not exceed 2.5 mg/day.

Cialis (for BPH or ED/BPH)

• PO (Adults): 5 mg once daily; Concurrent use of strong CYP3A4 inhibitors: Should not exceed 2.5 mg once daily.

Adcirca, Alyq, and Tadliq (for PAH)

• PO (Adults): 40 mg once daily; If receiving ritonavir for 1 wk: start 20 mg once daily; may then ↑ to 40 mg once daily based on tolerability; If initiating ritonavir while on Adcirca, Alyq, or Tadliq: stop Adcirca, Alyq, or Tadliq 24 hr before starting ritonavir; may reinitiate Adcirca, Alyq, or Tadliq at 20 mg once daily after 1 wk of therapy with ritonavir; may then ↑ to 40 mg once daily based on tolerability.

(Generic available)

• Tablets (Cialis): 2.5 mg; 5 mg; 10 mg; 20 mg;
• Tablets (Adcirca or Alyq): 20 mg;
• Oral suspension (Tadliq) (peppermint flavor): 20 mg/5 mL;
• In combination with: finasteride (Entadfi). See Appendix [not included in this PDA edition].

• Cialis for ED: Determine ED before administration. Tadalafil has no effect in the absence of sexual stimulation.
• Cialis for BPH: Assess for symptoms of BPH (urinary hesitancy, feeling of incomplete bladder emptying, interruption of urinary stream, impairment of size and force of urinary stream, terminal urinary dribbling, straining to start flow, dysuria, urgency) before and periodically during therapy.
• Digital rectal examinations should be performed before and periodically during therapy for BPH.
• Adcirca, Alyq, Tadliq: Monitor hemodynamic parameters and exercise tolerance prior to and periodically during therapy.

• PO: Administer dose as needed for ED at least 30 min prior to sexual activity; effectiveness may continue for 36 hr.
  • Administer dose for PAH, BPH, ED/BPH, or daily for ED once daily at the same time each day.
  • May be administered without regard to food. DNC: Swallow tablets whole; do not crush, break, or chew.
  • Shake suspension well for 30 sec before measuring dose.

• Instruct patient to take tadalafil as needed for ED at least 30 min before sexual activity and not more than once per day. Inform patient that sexual stimulation is required for an erection to occur after taking tadalafil. Instruct patient to take tadalafil for PAH as directed. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
• Advise patient that tadalafil is not indicated for use in women.
• Caution patient not to take tadalafil concurrently with alpha adrenergic blockers (unless on a stable dose) or nitrates. If chest pain occurs after taking tadalafil, instruct patient to seek immediate medical attention.
• Advise patient to avoid excess alcohol intake (5 units) in combination with tadalafil; may increase risk of orthostatic hypotension, increased heart rate, decreased standing BP, dizziness, headache.
• Instruct patient to notify health care professional promptly if erection lasts longer than 4 hr, if they are not satisfied with their sexual performance or develop unwanted side effects, or if they experience sudden or decreased vision loss in one or both eyes or loss or decrease in hearing, ringing in the ears, or dizziness.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Inform patient that tadalafil offers no protection against sexually transmitted diseases. Counsel patient that protection against sexually transmitted diseases and HIV infection should be considered.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

• Male erection sufficient to allow intercourse.
• Decrease in urinary symptoms of BPH.
• Increased exercise tolerance in PAH.

Adcirca, Alyq, Cialis, Tadliq