PDE5 inhibitors
Blocking PDE5 so cGMP builds up and smooth muscle relaxes.
Also called phosphodiesterase type 5 inhibitors and PDE-5 inhibitors.
Class card
- Drugs
- Sildenafil and Tadalafil
- Used for
- Erectile dysfunction
- Pulmonary arterial hypertension
- Urinary symptoms of BPH (tadalafil)
- Known for
- Headache
- Flushing of the face
- Blue-tinged or blurred vision
- Name stems
- -afil
3 cards: the class, and each drug in it.
Mechanism of action
How do PDE5 inhibitors work?
They inhibit phosphodiesterase type 5, the enzyme that breaks down cGMP in smooth muscle. During sexual stimulation nitric oxide raises cGMP in the corpus cavernosum; with PDE5 blocked, cGMP lasts longer, the muscle relaxes and blood flows in, but nothing happens without stimulation. The same effect widens the pulmonary arteries and reaches the smooth muscle of the prostate and bladder.
The drugs
PDE5 inhibitors with a card
- SildenafilIts low selectivity over retinal PDE6 (about 10-fold, against about 700-fold for tadalafil) is why blue-green color vision changes are typical of sildenafil.
- TadalafilIts long half-life gives a window of up to 36 hours and allows once-daily use for BPH; it is the only PDE5 inhibitor here licensed for BPH.
Uses
What are PDE5 inhibitors used for?
- Erectile dysfunction
- Pulmonary arterial hypertension
- Urinary symptoms of BPH (tadalafil)
Side effects
Side effects of PDE5 inhibitors
- HeadacheKnown for
- Flushing of the faceKnown for
- Blue-tinged or blurred visionKnown for
- Indigestion
- Stuffy nose
- Muscle aches and back pain
- Low blood pressure, dangerous with nitratesSerious
- PriapismSerious
- Sudden loss of vision (NAION)Serious
- Sudden loss of hearingSerious
What the class has in common. Each drug's card has its own, and Known for marks what an exam expects you to know.
Watch for
Cautions
- Never with nitrates in any form or with riociguat: blood pressure can fall dangerously.
- Not for men whose heart disease makes sexual activity unsafe; take care with alpha blockers and other antihypertensives.
- CYP3A4 inhibitors such as ritonavir raise their levels sharply.
- An erection lasting over 4 hours, or a sudden loss of vision or hearing, needs urgent assessment.
Remember them
A way to remember them
FLUSH
- F
- Flushing of the face
- L
- Loss of vision or hearing, sudden and rare
- U
- Upset stomach (indigestion)
- S
- Stuffy nose
- H
- Headache
Written for biofideX
Name stems
-afil means PDE5 inhibitor
Sildenafil, tadalafil and vardenafil block phosphodiesterase 5, which breaks down cGMP, so smooth muscle relaxes; erectile dysfunction is the best-known use.
- Every drug name stem
Don't mix them up
Classes easily confused with these
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Sildenafil citrate tablets for erectile dysfunction: label (DailyMed)
- Tadalafil tablets: label (DailyMed)
- Sildenafil tablets for pulmonary arterial hypertension: label (DailyMed)
- cGMP phosphodiesterase inhibitor (NCI Thesaurus)
- Sildenafil (NHS)
- Tadalafil (NHS)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Reproductive and urinary health
Practice PDE5 inhibitors with the other classes in this group: what each drug is, how it works, what it treats and what it's known for.
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