PDE5 inhibitors

Drugs that may be affected by PDE5 inhibitors include alpha-blockers, amlodipine, angiotensin II receptor blockers, bendroflumethiazide, enalaphl, metoprolol, nifedipine, nitrates, protease inhibitors. 

Drugs that may be affected by atazanavir include the following antiarrhythmics, atenolol, benzodiazepines, calcium channel blockers, cisapride, clarithromycin, ergot derivatives, HMG-CoA reductase inhibitors, immunosuppressants, indinavir, irinotecan, itraconazole, ketoconazole, oral contraceptives, PDE5 inhibitors, pimozide, rifabutin, saquinavir, tenofovir, tricyclic antidepressants, voriconazole, warfarin. 

Isosorbide Dinitrate Hydralazine (BiDil) [Antianginal, Antihypertensive/Vasodilator, Nitrate] Uses HF in African Amer-icans improve survival functional status, prolong time between hospitalizations Action Relaxes vascular smooth muscle peripheral vasodilator Dose Initially 1 tab tid PO (if not tol ated reduce to 1/2 tab tid), titrate >3-5 d as tolerated Max 2 tabs tid Caution [C, /-] recent MI, syncope, hypovolemia, hypotension, hep impair Contra For children, concomitant use w/ PDE5 inhibitors (sildenafil) Disp Tabs SE HA, dizziness, orthostatic hypotension, sinusitis, GI distress, tach, paresthesia, amblyopia Interactions t Risk of severe hypotension W/ antihypertensives, ASA, CCBs, MAOIs, phenothiazides, sildenafil, tadalafil, vardenafil, EtOH X pressor response Wf i -1- effects W7 NSAIDs EMS Use ASA, antihypertensives and CCBs w/ caution, may t hypotension concurrent Viagra-type drug use can lead to profound hypotension concurrent EtOH use can t effects OD May cause N/V, profound hypotension, skin flushing, HA from ICP, bradycardia, confusion, and circulatory collapse activated charcoal may be effective, epi use is contraindicated... 

Scheme 2.12. An optimized process for an intermediate of a PDE5 inhibitor.

Phosphodiesterase Type 5 (PDE5) inhibitors sildenafil citrate... 

A representative example of the coupling of furan derivatives is the preparation of the PDE5 inhibitor shown in 6.9. The concluding step in the synthesis was the Suzuki coupling of the 2-bromofuranc moiety with a series... 

PDE5 inhibitor PDE5 ICso (nM) tl/2 (h) Oral bioavailability (%) Approved doses (mg)... 

Caution [C, ] CrCl <30 Contra Component sensitivity, asthma, severe COPD, sinus bradycardia Disp Soln SE Irritation, bitter taste, superficial keratitis, ocular allergic Rxn EMS Drug is absorbed systemically OD May cause electrolyte disturbances (K), acidosis and bradycardia monitor ECG Doxazosin (Cardura, Cardura XL) [Antihypertensive/Alpha Blocker] Uses HTN symptomatic BPH Action < [-Adrenergic blocker relaxes bladder neck smooth muscle Dose HTN Initial 1 mg/d PO may be T to 16 mg/d PO BPH Initial 1 mg/d PO, may T to 8 mg/d XR 2-8mg qAM Caution [B, ] Use w/ PDE5 inhibitor (eg, sildenafil) can cause 1 BP Contra Component sensitivity Disp Tabs SE Dizziness, HA, drowsiness, sexual dysfxn, doses >4 mg T postural BP risk Interactions T Effects W/ nitrates, antihypertensives, EtOH i effects W/ NSAEDs, butcher s broom -t effects OF clonidine EMS Concurrent EtOH use can T drowsiness syncope may occur w/in 90 min of initial dose OD May cause profound hypotension place pt in supine position, give IV fluids, use pressors if needed... 

Sildenafil (Viagra, Revatio) [Vasodilator/PDE5 Inhibitor]... 

Mechanism of action of PDE5 inhibitors. Abbreviations NO, nitric oxide PDE5, phosphodieterase type 5. 

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