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Questions and Answers
Which medication is NOT used for acute migraine treatment?
What is the primary action of Acetazolamide?
Which class of medications have some prophylactic efficacy for migraines?
What is the main indication for Rho Kinase Inhibitors like Netarsudil?
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In which condition is Physostigmine probably NOT used?
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Which medication is indicated for severe thyrotoxicosis?
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Which beta blockers are exceptions to limited bioavailability due to hepatic first-pass effect?
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What impact does hepatic extraction saturation have on plasma levels of beta blockers?
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What is the primary effect of unopposed α1 receptor stimulation in ocular treatment?
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Which beta blocker is not appreciably metabolized in the liver?
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Which class of drugs is NOT considered a first-line treatment for hypertension?
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Which class of beta-blockers should have No significant membrane stabilizing activity (MSA) for ocular use?
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What is the result of the extensive hepatic first-pass effect on oral administration of beta blockers?
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What can occur if a cardioselective beta blocker is abruptly discontinued after long-term use?
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What effect do beta blockers have on myocardial infarction?
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Which of the following beta blockers is extensively metabolized in the liver?
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Which drug is specifically mentioned for the treatment of supraventricular tachyarrhythmias?
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Which drug class promotes aqueous outflow in glaucoma treatment?
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What phenomenon occurs in poor metabolizers after Metoprolol administration?
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What is the primary mechanism of action of cholinomimetics like Pilocarpine for glaucoma?
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Which of the following statements about beta blocker bioavailability is true?
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What effect do centrally acting α2 agonists have in the central nervous system?
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Which drug is classified as an alpha-2 selective agonist?
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Which of the following is likely to worsen a patient's condition if they have intrinsic sympathomimetic activity (ISA)?
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What happens to the plasma concentration of beta blockers at higher doses?
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Which beta-blocker is classified as cardioselective?
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Which beta blocker is specifically used for chronic heart failure?
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Which of the following beta blockers has low bioavailability due to extensive hepatic metabolism?
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What is a significant effect of alpha adrenergic agonists on intraocular pressure?
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What is a common side effect of using a centrally acting α2 agonist?
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What is a potential adverse effect of cholinomimetics in glaucoma treatment?
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In which condition would Phenytoin be less preferred due to its side effects?
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Which drug is known to decrease aqueous humor secretion?
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Which of the following drugs is NOT a carbonic anhydrase inhibitor?
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What is the therapeutic use of Timolol in glaucoma treatment?
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Which medication is specifically indicated for the prophylaxis of migraine?
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What is the primary mechanism by which propranolol decreases intraocular pressure in glaucoma?
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Which beta blocker is considered ultra-short acting with a rapid onset of action?
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Which beta blocker has a half-life of 3-4 hours?
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Which beta blocker is preferred for individuals with low cardiac reserve?
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What property does Atenolol have that affects its central nervous system (CNS) effects?
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What is a key pharmacokinetic characteristic of Esmolol?
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What is the major pharmacodynamic feature of Pindolol?
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Which beta blocker exhibits little interindividual variation in plasma concentrations?
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Which beta blocker lacks intrinsic sympathomimetic activity (ISA) and membrane stabilizing activity (MSA)?
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Study Notes
Metabolism of Beta Blockers
- Bioavailability varies, with exceptions like Betaxolol, Pindolol, Penbutolol, and Sotalol.
- P450 CYP2D6 genotype significantly influences individual metabolization and plasma clearance.
- Propranolol and Metoprolol have low bioavailability due to significant hepatic first-pass metabolism.
- As dose increases, plasma levels rise due to hepatic extraction saturation.
- Poor metabolizers can have 3-10 fold elevated plasma concentrations post-Metoprolol administration.
- Oral bioavailability is notably lower compared to IV administration.
Pharmacodynamics of Beta Blockers
- Beta blockers lower intraocular pressure (IOP) by decreasing cAMP production, aiding in treating ocular hypertension and glaucoma.
- Non-cardioselective blockers include Timolol, Levobunolol, Carteolol, and Metipranolol, while cardioselective options are Betaxolol and Levobetaxolol.
- Drugs utilized in treating angle-closure glaucoma need to be devoid of significant MSA or ISA to prevent negative effects.
- Withdrawals from beta blockers can result in rebound effects due to up-regulation of beta receptors.
Treatment Impact on Ocular Health
- α2 agonists (e.g., Brimonidine, Apraclonidine) and beta blockers significantly influence aqueous humor secretion.
- Cholinomimetics, Prostaglandin F2 alpha analogs, and Rho kinase inhibitors enhance aqueous outflow.
Drug Characteristics and Side Effects
- Atenolol is highly hydrophilic, minimizing CNS effects unlike other beta blockers.
- Pindolol is a nonselective drug with partial agonistic activity and low MSA, resulting in less bradycardia.
Therapeutic Uses of Beta Blockers
- Indicated for hypertension, angina pectoris, arrhythmias, myocardial infarction, and chronic heart failure management.
- Not first-line antihypertensive treatment, as ACE inhibitors and ARBs are preferred.
- Can prevent migraines but are ineffective in treating acute migraine episodes.
Additional Clinical Insights
- Propranolol can be effective for acute anxiety states and essential tremor.
- Beta blockers can aid in managing severe thyrotoxicosis, especially in thyroid storm situations.
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Description
This quiz focuses on the metabolism of beta blockers and discusses key factors affecting their bioavailability. It highlights the significance of the P450 CYP2D6 genotype and its role in interindividual differences in plasma clearance rates, along with exceptions to these rules.
