Bitter blockers

Bitter blockers and sweetness potentiators are another field of current importance. 

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... 

Simple lignans involving a Phe-C -C -Phe structure are illustrated by the antioxidant and Ca2+ channel blocker nordihydroguaiaretic acid (NDGA) (3,4-dihydroxyphenyl-CH2-CH(CH3)-CH(CH3)-CH2-(3, 4 -dihydroxyphenyl)), the bitter-tasting phyllanthin and the cAMP phosphodiesterase inhibitor ar-hinokiresinol. Simple lignans of the C3—Phe—Phe—C3 kind are illustrated by the antibacterials honokiol and the protein kinase inhibitor magnolol. 

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