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23 Cards in this Set

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  • Back
What two drugs have assymetric centers?
Teproxide and Captopril
what is an important characteristic of terproxide
it is a natural product isolated from pit-venom snake and it has a pyroglutamic acid at pos #1
What drugs have L-S configuration
Captopril and Nimodipine
what are two other characteristics for Captopril
it has much higher affinity for angiotenisn and the sulfur ties up zinc.
What are characteristiics of Enalipril
polarity is high, it forms ester-GI absorbtion is high, and phenylethyl enchances binding.
what is one characteristic of ramiprilat
it has increased bioavailabilty
characteristics for MOexiprilat
it is 1000x more active-more polar
what is more potent than enalapril
Benazepril
Which drugs generate no active metabolism?
Candesartan, Irbesartan, and Bepridil
what is one characteristic of Telmarsartan?
hydroxylating the methyl require CYP 450
What is an characteristic of Losartan K+
metabolize to COOH- 4x more active than parent drug
What is one charact for Valsartan
only ABR that is not a prodrug
one charact for Eprosartan
bind both pre and post
What includes the Phenylaklyamines
Verapamil and Bepridil
what are the charact for Verapamil
it is taken orally ER and has low bioavaibliity, generates 12 active metabolites
What are the characteristics for Bepridil?
has omega-1 oxidation, forms N-oxide and can cause arrhytmias
What includes the Benzothiazines
Diltiazem
What is the net sign of rotation for the dilitizem
dextro
how is Dilitizem opposite from verapamil
it has a much higher bio and has SR
what are important metabolic qualities for diltizem?
N-demythaltion still active, but clinically insignificant.
contains about 50% of activity of parent
what are the requirements for Dihydropyridines?
esters push the 2nd ring out of the plane
if cmp was basic enough to form a salt, it would not be active
Ring at C4 is essential
esters at 3,5
what are the characteristics for nefedipine
nitro gp to ensure its out of plane, all metabolites are inactive
What are characteristics for Nimodipine
it prevents vasospams, and is specically for cerebral edema.
crosses BBB