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35 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Does Prozasin have a high or low first pass effect?
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High
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What is the receptor affinity for this antagonist Phenoxybenzamine? Action? Tx? When does it decrease BP the most? it it revesible?
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Phenoxybenzamine: (1) Affinity: IRREVERSIBLE ∂ antagonist: ∂1>∂2… (2) Action: (a) blocks reuptake of NE… (b) decreases BP when sympathetic tone is high…
(3) Tx: Pheochromocytoma, reduces BP in standing position |
None
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What are the 5 ADR of Phenoxybenzamine?
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postural hypotension, tachycardia, nasal stuffiness, inhibits ejaculation, CNS effects (enters brain)
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Name the 3-∂ antagonist and the one -∂-agonist?
Which one of these enters the CNS? Which one is a prodrug? |
Phentolamine, Prozasin, Phenoxybenzamine, Midodrine
2) Phenoxybenzamine enters the CNS 3) Midodrine is a prodrug |
None
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Name the 5 ß-blocking drugs.
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Proproanolol, pindolol, meoprolol, atenolol and labetalol
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None
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Name the one combination ß1/ß2/∂1 blocking drug.
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Carvedilol
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None
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Which of the alpha antagonists is irreversible?
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Phenoxybenzamine
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What is the receptor affinity for this AGONIST Midodrine? Action? Tx?
Is there CNS activity? |
Midodrine… This is an AGONIST:
(1) Affinity: Selective ∂1 AGONIST Selective ∂1… (2) Action: Prodrug… No ß adrenergic activity, No NE release stimulation, no CNS activity… (3) Tx: hypotensin (4) No CNS activity |
None
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Out of these drugs which is the prodrug, and (2) which would potentiate antidepressant durgs?: Phentolamine, Prozasin, Phenoxybenzamine, Midodrine, Proproanolol, pindolol, meoprolol, atenolol, labetalol, carvedilol
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(1) Prodrug: Midodrine… (2) Potentiate antidepressants: Pindolol
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What are Midodrine's ADR and contraindications?
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Midorines ADR: Supine hypertension if given at night… (1) Contraindicated: diabetes because ∂ agonists increase glucogenesis
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None
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What is the receptor affinity for this antagonist Phentolamine? Action? Tx? Diagnostic use? ADR?
Which of the ∂ antagonists is IRREVERSIBLE? |
Phentolamine:
(1) Affinity: Pure Competitive ∂ antagonist ∂1=∂2: (2) Action: (a) decrease peripheral resistance (w/o ∂1)… (b) increase NE release (w/o ∂2)… (3) Tx: (a) pheochromocytoma (excessive release of catacholamines due to adrenal tumor) (b) erectile dysfunction. (4) diagnosis of pheochromocytoma (patients w/ tumor have a greater drop in pressure than those w/ primary HTN. (5) May cause baroreceptor mediated tachycardia... nasal congestion (6) Phenoxybenzamine |
None
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Which of the alpha antagonists is used for BPH?
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Prozasin
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What is the receptor affinity for this antagonist Propranolol? Action? Tx?
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Propranolol: (1) Affinity: Pure competitive ß antagonist… (2) Action: ß antagonist… (3) Tx: HTN, anginia, V-arrythmia, MI, pheochromocytoma, migraine prophylaxis…
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What are the 3 ADR of Phentolamine?
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reflex tachycardia, nasal congestion, orthostatic hypotension
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Out of these drugs which are (1) partial agonists and (2) which has a low bioavailability: Phentolamine, Prozasin, Phenoxybenzamine, Midodrine, Proproanolol, pindolol, metoprolol, atenolol labetalol, carvedilol…
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(1) Partial agonists: pindolol, Labetalol… (2) low bioavailability: Propranolol
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None
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What are the ADRs of Propranolol? What are the contraindications?
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Propranolol: ADRs: bradycardia, neg inotrope, decreased CO, bronchoconstriction, exercise intolerance, fatigue, sleep disturbance… (2) counterindications: diabetes melitus due to ß response to hypoglycemia is stunted
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Which of the alpha drugs is a prodrug?
Which alpha drug enters the CNS/brain? |
Midodrine is a prodrug
Phenoxybenzamine enters the CNS |
None
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What is the receptor affinity for this antagonist Prazosin? Action? Tx?
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Prazosin: (1) Affinity: highly selective competitive ∂1 antagonist… (2) Action: relaxes smooth muscle of vasculature and prostate… (3) Tx: HTN and BPH
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Propranolol: what is its bioavailability? Where is it metabolized? Is its therapeutic index wide or narrow?
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Propranolol: Bioavailability: 26%… Metabolized in gut… Narrow therapeutic index
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Of the ß blockers, which do not have membrane stabilizing activity?
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Atenolol and Metoprolol
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Which of the alpha drugs blocks reuptake of NE?
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phenoxybenzamine
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Which 2 of the alpha antagonists are used for Pheochromocytoma?
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Phentolamine, phenoxybenzamine
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What is the receptor affinity for this antagonist Pindolol? Action? Tx? ADR?
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Pindolol:
(1) Affinity:- Pure competitive β-antagonist/PARTIAL AGONIST. (2) Action: Antagonist: in presence of intrinsic agonist (b) PARTIAL AGONIST in absence of intrinsic agonist… (3) Tx: HTN, angina. (4) May potentiate antidepressant meds (D) |
None
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Which of the alpha antagonists are used HTN?
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Prozasin and Phenoxybenzamine
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What is the receptor affinity for this antagonist Metoprolol? Action?
What are 5 main uses for this drug???? |
Metoprolol: (1) Affinity: Pure β1-antagonist… (2) Action: (a) No ISA or membrane stabilizing activity… (b) Slightly lipophilic… (3) Tx: stable angina, CHF, HTN, migraines, MI
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None
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Which of the alpha antagonists is used for erectile dysfunction?
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Phentolamine
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What is Metoprolol contraindicated in?
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Metoprolol Contraindication: acute MI tx, high order heart block tx… (debatable: β blockers preferred in those with diabetes or peripheral vascular disease)
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None
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What is the receptor affinity for this antagonist Atenolol? Action? Tx?
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Atenolol: (1) Affinity: Competitive β1 antagoinist… (2) Action: No ISA or MSA… (3) Tx: HTN
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None
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Which of the alpha antagonists can be used to diagnose pheochomocytoma?
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Phentolamine
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Which of the alpha antagonists will cause a decrease in BP when sympathetic tone is highest?
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Phenoxybenzamine
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What are the contraindications for Atenolol?
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Atenolol Contraindicated: Better beta blocker for diabetes or peripheral vascular disease patients (β2 blocker bad)
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Which drugs are contraindicated for Diabetes? Why?
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Midodrine (Contraindicated: diabetes because ∂ agonists increase glucogenesis)… ß-blocking drugs (counterindications: diabetes melitus due to ß3 response to hypoglycemia is stunted)… At
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What is the receptor affinity for this antagonist Labetalol? Action? Tx?
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Labetalol: (1) Affinity:
(a) Competitive β antagonist/parial agonist@ ß receptors (b) α1 antagonist… (2) Action: racimic mixture… ISA at β receptors… (3) Tx: HTN |
None
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What is the ADR of Labetalol?
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Labetalol ADR: hepatic failure
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What is the receptor affinity for this antagonist Carvedilol? Action? Tx?
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"Carvedilol: (1) Affinity: Blocks β1, β2, α1…
(2) Action: has antioxidant, antiproliferative effects, No ISA, Can vasodilate... (3) Tx: CHF |
None
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