TADALAFIL
THERAPEUTICS
Class
- Phosphodiesterase-5 inhibitor (PDE-5 inhibitor)
TADALAFIL commonly prescribed for
(Bold for FDA approved)
How TADALAFIL works
• PDE-5 is responsible for degradation of cyclic guanosine monophosphate (cGMP); cGMP produces smooth muscle relaxation in the corpus cavernosum and allows inflow of blood.
• Inhibition of PDE-5 causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum.
How long until TADALAFIL works
• Maximum observed plasma concentrations are reached within 30 minutes to 6 hours (median 2 hours) of oral dosing
SIDE EFFECTS
Notable Side Effects
• Headache
• Flushing
• Nasal congestion
• Dyspepsia (indigestion)
• Back pain and muscle aches
• Dizziness
• Blurred vision or changes in color vision
Life Threatening Side Effects
• Hypotension, especially when taken with nitrates or alpha-blockers
• Priapism (prolonged erection lasting more than 4 hours)
• Rare cardiovascular events such as myocardial infarction or stroke (often linked to pre-existing conditions)
weight gain

unusual
sedation

unusual
What to do about TADALAFIL side effects
• Reduce dose
DOSING AND USE
usual dosage range
• Erectile Dysfunction (as-needed use)
• 10 mg taken prior to anticipated sexual activity, at least 30 minutes before.
• Dose can be increased to 20 mg or reduced to 5 mg based on efficacy and tolerability.
• Maximum frequency: once per day.
• Erectile Dysfunction (daily use) 2.5 mg to 5 mg once daily, taken at the same time each day.
• Benign Prostatic Hyperplasia (BPH) 5 mg once daily, taken at the same time each day.
• Pulmonary Arterial Hypertension (PAH) 40 mg (two 20 mg tablets) once daily.
Dosage Forms
• Tablets of 2.5 mg, 5 mg, 10 mg, and 20 mg
long term use
• Safe
habit forming
• No
SPECIAL POPULATIONS
Renal Impairment
• No adjustment for mild to moderate impairment
• For patients with severe impairment, consider a starting dose of 2.5 mg
Hepatic Impairment
• Consider a starting dose of 2.5 mg
Cardiac Impairment
• Elicits vasodilatory properties, resulting in mild and transient decreases in blood pressure
• Treatment for erectile dysfunction generally should not be instituted in men for whom sexual activity is inadvisable because of their underlying cardiovascular status
• There are no controlled clinical data on the safety or efficacy of sildenafil in patients who have suffered a myocardial infarction, stroke, or life-threatening arrhythmia within the last 6 months; have resting hypotension (BP <90/50 mmHg) or hypertension (BP >170/110 mmHg); or have cardiac failure or coronary artery disease causing unstable angina; use only with caution in these patients
• Use with caution in patients with left ventricular outflow obstruction (e.g., aortic stenosis, idiopathic hypertrophic subaortic stenosis) and those with severely impaired autonomic control of blood pressure
Elderly
• Some patients may tolerate lower doses better
• Consider a starting dose of 2.5 mg
Children and Adolescents
• Not recommended for use in pediatric patients
• Safety and efficacy have not been established
Pregnancy
• Not indicated for use in women
• Controlled studies have not been conducted in pregnant women.
Breast Feeding
• Some drug is found in mother’s breast milk
Based on data Published online by Cambridge University Press
Compiled by Dr. Jash Ajmera