Phosphodiesterase inhibitors
| Types | Active ingredient | Indications | Mechanism of action | Desired effect |
| Nonspecific phosphodiesterase inhibitors ... | Theophylline (methylxanthines) | COPD (severe and refractory cases) Asth ... | Nonspecific PDE inhibition → ↓ hydrolysi ... | Inhibition of proinflammatory mediators ... |
| Phosphodiesterase type 5 inhibitor (PDE5 ... | Sildenafil Tadalafil Avanafil Vardenafil ... | Erectile dysfunction Pulmonary hypertens ... | PDE5 inhibition → ↓ breakdown of cGMP → ... | Decrease in pulmonary vascular resistanc ... |
| Phosphodiesterase type 4 inhibitor (PDE4 ... | Roflumilast | Severe COPD | PDE4 inhibition → ↑ cAMP in bronchial ep ... | Inhibition of proinflammatory mediators ... |
Which is the best PDE5 inhibitor?
- Horny Goat Weed (blocks PDE5 and boosts libido, which the ED drugs do not do)
- Artichoke Extract (another inhibitor that also reduces aromatase)
- Forskolin (this acts as an anti-aromatase as well)
- Quercetin (elevates GMP threefold according to a study published in the British Journal of Pharmacology)
Does Viagra inhibit phosphodiesterase?
The four oral PDE5inhibitors commercially available in the U.S. are sildenafil (Viagra, Pfizer), vardenafil (Levitra and Staxyn, Bayer/GlaxoSmithKline), tadalafil (Cialis, Eli Lilly), and a more recently approved drug, avanafil (Stendra, Vivus).
What are prostaglandin inhibitors?
Prostaglandin inhibitors may cause stomach ulcers. Prostaglandin inhibitors are drugs that act on lipid compounds known as prostaglandins, found throughout the body to regulate muscle contractions and related activities. The body produces them locally, and while they are chemical messengers, they are not classified as hormones.
What are DPP-4 inhibitors for type 2 diabetes?
DPP-4 inhibitors are a class of prescription medicines that are used with diet and exercise to control high blood sugar in adults with type 2 diabetes. Medicines in the DPP-4 inhibitor class include sitagliptin, saxagliptin, linagliptin, and alogliptin.
What does phosphodiesterase inhibitor do?
Phosphodiesterase inhibitors are a class of medications that interfere with certain types of chemical reactions in your blood. This helps blood vessels relax, reduces inflammation and more.
What is the most commonly used phosphodiesterase inhibitor?
What are some examples of common phosphodiesterase inhibitors? PDE5 inhibitors are the most common and include sildenafil, tadalafil, vardenafil, and avanafil. The most common PDE4 inhibitors are roflumilast, apremilast, and ibudilast. Some examples of PDE3 inhibitors are cilostazol and milrinone.
Is Viagra a phosphodiesterase inhibitor?
One of the mainstays of ED treatment is the oral phosphodiesterase type 5 (PDE5) inhibitor class. The four major PDE5 inhibitors are sildenafil (Viagra), tadalafil (Cialis), vardenafil (Levitra), and avanafil (Stendra).
Is coffee a phosphodiesterase inhibitor?
Recent reports that coffee can significantly inhibit cAMP phosphodiesterases (PDEs) in vitro, as well as in vivo, have described another beneficial effect of coffee consumption. However, the PDE-inhibiting substances remain mostly unknown.
Is caffeine a phosphodiesterase inhibitor?
However, caffeine is a fairly weak inhibitor of phosphodiesterase enzymes, and the in vivo concentrations at which behavioral effects occur are probably too low to be associated with meaningful phosphodiesterase inhibition (Burg and Werner, 1975; Daly, 1993).
What happens if a woman takes Cialis?
We know that in men, Viagra dilates blood vessels and increases the flow of blood to the penis. Women who take it might also have increased blood flow to the genitals. That may help increase sensitivity, arousal, and orgasmic function. Studies on its effectiveness in women have had mixed results.
What happens if a female takes Viagra?
There is anecdotal evidence that Viagra may increase sexual pleasure in women. We know that Viagra works in men by increasing the blood flow to the penis. In women it's thought that Viagra could increase blood flow to the female genital area, increasing lubrication and aiding orgasm.
Which drugs can cause erectile dysfunction?
Thiazides are the most common cause of erectile dysfunction among the high blood pressure medicines....Cimetidine (Tagamet)Dimenhydrinate (Dramamine)Diphenhydramine (Benadryl)Hydroxyzine (Vistaril)Meclizine (Antivert)Nizatidine (Axid)Promethazine (Phenergan)Ranitidine (Zantac)
When do we use phosphodiesterase inhibitors for men?
Phosphodiesterase type 5 (PDE5) inhibitors are a group of medications most commonly used to treat erectile dysfunction (ED). Their ability to improve symptoms of ED was discovered accidentally while researchers were examining their potential use for high blood pressure and angina.
What is sildenafil used for?
Sildenafil is used to treat men who have erectile dysfunction (also called sexual impotence). Sildenafil belongs to a group of medicines called phosphodiesterase 5 (PDE5) inhibitors. These medicines prevent an enzyme called phosphodiesterase type-5 from working too quickly.
What do phosphodiesterase type 5 inhibitors do?
The phosphodiesterase type 5 (PDE5) inhibitors cause vasodilation in the penis and lung by blocking the breakdown of cyclic guanosine monophosphate (cGMP) which results in prolongation of the action of mediators of vasodilation including nitric oxide (NO).
Which of the following is a PDE inhibitors?
Sildenafil, vardenafil, tadalafil, and avanafil are classified as PDE5 inhibitors and are indicated for the treatment of men with ED. Sildenafil, the first PDE5 inhibitor, was introduced in 1998. More than 20 million men were treated with sildenafil in its first 6 years on the market.
What is a phosphodiesterase inhibitor?
Phosphodiesterase inhibitors are a class of medications that promote blood vessel dilation (vasodilation) and smooth muscle relaxation in certain p...
How do phosphodiesterase inhibitors work?
Phosphodiesterase inhibitors work by inhibiting the phosphodiesterase enzymes, thus preventing them from breaking down cAMP and cGMP molecules in t...
What happens when phosphodiesterase is inhibited?
When phosphodiesterase is inhibited, it is not able to break down the cAMP and cGMP. Thus, their levels inside the cell increase, which in turn lea...
What are phosphodiesterase inhibitors used for?
Phosphodiesterase inhibitors are classified based on which specific phosphodiesterase enzyme they target. There are 11 families of phosphodiesteras...
What are some examples of common phosphodiesterase inhibitors?
PDE5 inhibitors are the most common and include sildenafil, tadalafil, vardenafil, and avanafil.The most common PDE4 inhibitors are roflumilast, ap...
Is Viagra a phosphodiesterase inhibitor?
Viagra is a PDE5 inhibitor most often used for the treatment of erectile dysfunction. Viagra has also been useful in the treatment of pulmonary hyp...
Are phosphodiesterase 5 inhibitors a competitive inhibitor?
Phosphodiesterase type 5 inhibitors are competitive and reversible inhibitors. When a PDE5 inhibitor is used, it competitively binds to PDE5 to sto...
Is caffeine a phosphodiesterase inhibitor?
Caffeine is a phosphodiesterase inhibitor that has been shown to increase the levels of cAMP in the cell thus leading to smooth muscle relaxation....
Are methylxanthines phosphodiesterase inhibitors?
Methylxanthines are among the first phosphodiesterase inhibitors to be discovered, and are nonspecific. The most common methylxanthine is theophyll...
What are the side effects of phosphodiesterase inhibitors?
Common side effects of PDE5 inhibitors include headache, nasal congestion, dyspepsia and flushing. A potential rare side effect of PDE5 inhibitors...
What is phosphodiesterase inhibitor?
Phosphodiesterase inhibitors are a class of medications that promote blood vessel dilation (vasodilation) and smooth muscle relaxation in certain parts of the body, such as the heart, lungs, and genitals . Phosphodiesterases are a diverse family of enzymes that play a key role in regulating cell functions by indirectly increasing ...
What is the role of phosphodiesterases in the cell?
Phosphodiesterases are a diverse family of enzymes that play a key role in regulating cell functions by indirectly increasing the intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), both of which are “second messengers” that regulate the primary effects of hormones and neurotransmitters.
What is the difference between PDE5 and PDE4?
Additionally, PDE5 inhibitors trigger pulmonary vasodilation, helping to regulate the pulmonary perfusion and pressure, thu s they can be used to treat pulmonary hypertension when given at a lower dose compared to erectile dysfunction. PDE4 inhibitors. PDE4 inhibitors work by increasing the levels of cAMP.
What is the purpose of PDE5 inhibitors?
PDE5 inhibitors are commonly used for the treatment of erectile dysfunction and pulmonary hypertension.
How do nonspecific inhibitors work?
Nonspecific inhibitors work by decreasing the destruction of the cAMP by any phosphodiesterase enzyme. They mainly induce mild dilation of the bronchioles of the lungs and help reduce airway inflammation. Nonspecific phosphodiesterase inhibitors are used in the treatment of chronic obstructive pulmonary disease, as well as for short term and long term management of asthma.
What is PDE3 inhibitor?
In addition, PDE3 inhibitors can prevent platelet aggregation into clots, and can thus be used to prevent and treat myocardial infarction ( heart attack ).
How many families of phosphodiesterase inhibitors are there?
Phosphodiesterase inhibitors are classified based on which specific phosphodiesterase enzyme they target. There are 11 families of phosphodiesterase enzymes and PDE inhibitors for each. Among these, the most widely used are four types of phosphodiesterase inhibitors: phosphodiesterase type 5 inhibitors ( PDE5 inhibitor ), phosphodiesterase type 4 inhibitors (PDE4 inhibitor), phosphodiesterase type 3 inhibitors (PDE3 inhibitor), and nonspecific inhibitors.
What is phosphodiesterase inhibitor?
Phosphodiesterase inhibitors are class medications used in the management and treatment of chronic obstructive pulmonary disease (COPD), erectile dysfunction (ED), pulmonary arterial hypertension (PAH), benign prostatic hyperplasia (BPH), a cute decompensated heart failure, psoriasis, psoriatic arthritis (PA), a topic dermatitis (AD), and neonatal apnea. In the class of medications that prevent cAMP and/or cGMP degradation, it exhibits smooth muscle relaxation, vasodilatory, and bronchodilatory effects. This activity outline and describes the indications, action, and contraindications for phosphodiesterase inhibitors as a valuable agent in the management of chronic obstructive pulmonary disease (COPD), erectile dysfunction (ED), pulmonary arterial hypertension (PAH), acute decompensated heart failure, psoriasis, psoriatic arthritis (PA), and other disorders when applicable. This activity will highlight the mechanism of action, adverse event profile, and other key factors (e.g., off-label uses, dosing, monitoring, relevant interactions) pertinent for members of the interprofessional team in the management and care of patients with chronic obstructive pulmonary disease (COPD), erectile dysfunction (ED), pulmonary arterial hypertension (PAH), and related conditions.
What is PDE-4 inhibitor?
PDE-4 is an enzyme found in cells of the lungs, and PDE-4 inhibitors inhibit the degradation of intracellular cyclic adenosine monophosphate (cAMP) and increase cAMP levels in target cells, further causing bronchial muscle relaxation. Along with its effects on the lungs, it also decreases pro-inflammatory mediators. [1] These agents are useful in treating COPD, psoriatic arthritis (PA), and atopic dermatitis (AD). Crisaborole is a PDE-4 inhibitor indicated for mild to moderate atopic dermatitis, and its mechanism of action of its therapeutic effect is not fully understood.
What is the difference between pentoxifylline and ibudilast?
Pentoxifylline is a xanthine analog and is a non-selective phosphodiesterase inhibitor, FDA approved in 1984 for muscle pain caused by intermittent claudication in chronic peripheral arterial disease. Anagrelide is a PDE-3 inhibitor approved for the treatment of thrombocythemia caused by myeloproliferative disorders. Ibudilast is a non-selective PDE inhibitor that has not secured approval by the FDA for its use. Ibudilast action causes dilations of the bronchioles and has been used to treat asthma in Japan since 1989. [9] [10] The agent is also said to cross the blood-brain barrier, exert anti-inflammatory actions in the central nervous system, and maybe a hopeful agent for inflammatory neurological disorders. [9] [10] Caffeine, one of the most popularly utilized psychoactive compounds used globally, also inhibits phosphodiesterase as one of its three mechanisms of action. It is labeled generally recognized as safe (GRAS) by the FDA since 1958. [11] [12] Caffeine is a CNS stimulant used for fatigue, drowsiness, enhancing memory, cognition, and performance. [12] [11] Caffeine citrate has been used to treat apnea of prematurity in neonates gestation age of twenty-two weeks to less than thirty-three weeks and received approval in 1999 for its use.
What is the most common PDE inhibitor?
Among the phosphodiesterase inhibitors, sildenafil is the more common agent acting on PDE-5 and is FDA-approved in 1998 for erectile dysfunction. [3] Sildenafil use is not limited to the treatment of erectile dysfunction (ED) and obtained FDA approval in 2005 to treat pulmonary arterial hypertension (PAH) in adults. [4] The use of sildenafil in pediatric populations for pulmonary arterial hypertension (PAH) has not received approval and is considered off-label use. [5] Vardenafil and avanafil are other PDE-5 inhibitors, also approved for erectile dysfunction (ED). Tadalafil is a PDE-5 inhibitor approved to treat benign prostatic hyperplasia (BPH) and erectile dysfunction (ED). As both conditions may coincide in the later durations of life, tadalafil may be used as monotherapy for its therapeutic use to treat both conditions. [6]
Is Cilostazol contraindicated for heart failure?
Cilostazol: Heart failure is an absolute contraindication to cilostazol use.
Is PDE-4 a toxic drug?
PDE-4 inhibitor theophyl line serum concentrations of more than 20 mcg/mL are in a toxic range. [33] Theophylline-induced seizures and arrhythmias prompt treatment immediately as it may result in mortality from hemodynamic compromise at serum concentrations of 30 mcg/mL or greater. Therapy with anticonvulsants such as benzodiazepine and antiarrhythmic treatment should start immediately. PDE-5 and PDE-3 inhibitors undergo hepatic metabolism, and inhibitors of CYP3A4 or CYP2C19 can increase the serum drug concentrations of therapy. Dose modifications are required before the initiation of treatment to avoid adverse effects.
Is pentoxifylline a phosphodiesterase inhibitor?
Theophylline is a nonspecific phosphodiesterase inhibitor used to treat COPD, and the mechanism of action is not entirely understood. [19] Although not fully understood, pentoxifylline's mechanism of action is believed to act by the nonselective inhibition of phosphodiesterase enzymes similar to theophylline. This action further enhances blood flow and perfusion in the limbs by increased erythrocyte flexibility, decreased blood viscosity, decreased cell proliferation, and reduced inflammation. This mechanism allows pentoxifylline to be used therapeutically in patients suffering from muscle aches and pain associated with peripheral arterial disease. [20] [21]
Why do people take PDE5 inhibitors?
This inhibition relaxes the blood vessels and increases blood flow. People may take PDE5 inhibitors to treat erectile dysfunction or pulmonary hypertension. In people with erectile dysfunction, PDE5 inhibitors increase blood flow to the penis, improving erectile function.
What is the effect of PDE5 inhibitors on blood vessels?
PDE5 inhibitors block PDE5, an enzyme in the walls of blood vessels. Blocking PDE5 causes blood vessels to relax, increasing blood flow to certain areas of the body.
What is the effect of PDE5 on blood flow?
PDE5 is an enzyme in the walls of blood vessels. It affects blood flow and how cells signal within the body. PDE5 inhibitors block the PDE5 enzyme to prevent it from working. This inhibition relaxes the blood vessels and increases blood flow.
How does PDE5 help with hypertension?
In people with pulmonary hypertension, PDE5 inhibitors can help by: controlling blood flow to the arteries in the lungs. increasing blood flow to the lungs. lowering blood pressure. Research. Trusted Source. also suggests that PDE5 inhibitors may be helpful in treating heart disease, diabetes, and cancer.
What is Levitra used for?
vardenafil (Levitra), for the treatment of erectile dysfunction
What are the side effects of PDE5?
have a history of heart failure or angina. are currently using alpha-blockers. Common, and usually mild, side effects of PDE5 inhibitors can include: headaches. flushing.
Is PDE5 harmful?
PDE5 inhibitors can also potentially be harmful to people with certain conditions. Before taking these medications, a person should make their doctor aware if they:
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Summary
Phosphodiesterase inhibitors ( PDE inhibitors) are a class of drugs that inhibit phosphodiesterase enzymes ( PDE enzymes). PDE enzymes normally break off phosphate groups and decrease cAMP or cGMP in target cells . PDE inhibitors are classified according to which enzyme (s) they act upon as nonspecific, PDE5, PDE4, and PDE3 inhibitors. PDE5 inhibitors cause pulmonary vasodilation and penile smooth muscle relaxation, and are used for pulmonary hypertension and erectile dysfunction .
Pharmacodynamics
Phosphodiesterase ( PDE ) inhibitors are a heterogenic class of drugs that target various isoforms of PDE enzymes. Normally, the PDE decreases cAMP or cGMP in target cells by catalyzing the hydrolysis of these second messengers . By inhibiting this step, PDE inhibitors actually increase cAMP and/or cGMP concentrations.
What are Selective phosphodiesterase-4 inhibitors?
Selective phosphodiesterase-4 inhibitors increase cyclic adenosine-3′,5′-monophosphate (cAMP) levels, resulting in a broad spectrum of anti-inflammatory effects in almost all inflammatory cells.
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
What enzyme breaks down cyclic GMP molecules and reverses the erection process?
An enzyme called PDE5 breaks down cyclic GMP molecules and reverses the erection process. However, PDE5 inhibitors are similar in structure to cyclic GMP and bind to PDE5 to block this breakdown. This action enhances the action of NO and helps promote blood flow.
Is Malculra pomifera a PDE5 inhibitor?
Research has found that derivatives of these isoflavones may be a potential lead for future PDE5-inhibitor development .
