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An example of this is the repurposing of the antimineralocorticoid and diuretic spironolactone, which was found to produce feminization and gynecomastia as side effects, for use as an antiandrogen in the treatment of androgen-dependent conditions like acne and hirsutism in women. [1] Metformin also causes off-target activity. [citation needed]
Administration can prevent common side-effects, such as nausea and vomiting, as a result of interaction with D 2 receptors in the vomiting center (or cheomoreceptor trigger zone) located outside the blood–brain barrier. [2] Examples of extracerebral decarboxylase inhibitors include carbidopa and benserazide.
The substituted phenyl group at the top of the channel interacts with the side-chains of amino acid residues through hydrophobic and electrostatic interactions. Tyr385 makes for some sterical restrictions of this side of the binding site so a small substituent of the phenyl group makes for better binding. Degrees of freedom are also important ...
There are two drug-binding α 2 δ subunits, α 2 δ-1 and α 2 δ-2, and most gabapentinoids show similar affinity for (and hence lack of selectivity between) these two sites. [1] In most cases, gabapentinoid drugs do not seem to directly alter the action of VGCC and instead reduce the release of certain excitatory neurotransmitters. [2 ...
Description: Side effects of spironolactone (25–400 mg/day) with ≥1% incidence in a 2017 hybrid systematic review of clinical studies of spironolactone for acne in women. Side effects with <1% incidence included postural hypotension, depression, diarrhea, muscle pain, increased appetite, drowsiness, rashes/drug eruptions, chloasma-like skin ...
Muscarinic antagonist effects and muscarinic agonist effects counterbalance each other for homeostasis. Certain muscarinic antagonists can be classified into either long-acting muscarinic receptor antagonists ( LAMA s) or short-acting muscarinic receptor antagonists ( SAMA s), depending on when maximum effect occurs and for how long the effect ...
Steroidal aromatase inhibitors are a class of drugs that are mostly used for treating breast cancer in postmenopausal women. High levels of estrogen in breast tissue increases the risk of developing breast cancer and the enzyme aromatase is considered to be a good therapeutic target when treating breast cancer due to it being involved in the final step of estrogen biosynthetic pathway and also ...
A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. [1] There are three receptors of the gamma-aminobutyric acid. The two receptors GABA-α and GABA-ρ are ion channels ...