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