Pharmacological Differences of Beta Blockers Quiz

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Questions and Answers

Which of the following is a leukotriene receptor antagonist?

Zileuton

Zafirlukast (correct)

Salmeterol

Fluticasone

What is the primary mechanism of action of long-acting beta2-agonists (LABAs) in bronchial smooth muscle?

Inhibit 5-lipoxygenase enzyme

Inhibit release of histamine and leukotrienes

Block leukotriene receptors

Stimulate ATP and cAMP, leading to bronchodilation (correct)

Which receptor subtype is predominant in the heart?

Beta1-receptors (correct)

Alpha-receptors

Beta2-receptors

Leukotriene receptors

Which of the following is a long-acting beta2-agonist (LABA)?

Salmeterol Signup and view all the answers

Which drug class is associated with Schedule II classification by the DEA?

Opioid analgesics and stimulants Signup and view all the answers

Which of the following statements about beta2-agonists is true?

They are primarily used as bronchodilators Signup and view all the answers

Which beta blocker is specifically indicated for glaucoma?

Levobunolol Signup and view all the answers

Among the listed agents, which one has intrinsic sympathomimetic action?

Oxprenolol Signup and view all the answers

Which beta blocker has both membrane stabilizing effect and antioxidant effect?

Carvedilol Signup and view all the answers

Which agent is specifically indicated for migraine prophylaxis?

Timolol Signup and view all the answers

Among the listed agents, which one is used for the control of tremor, portal hypertension, and esophageal variceal bleeding?

Propranolol Signup and view all the answers

Which beta blocker has greater aqueous solubility?

Carteolol Signup and view all the answers

Which type of drugs are not absorbed from the gut?

Lipid-insoluble and water-insoluble drugs Signup and view all the answers

What is the primary method through which 90% of drugs are absorbed?

Passive diffusion (non-ionic diffusion) Signup and view all the answers

Which drug has 0% protein binding?

Lisinopril Signup and view all the answers

What type of binding lessens the amount of a drug at the active site?

High protein binding Signup and view all the answers

Which form of drug can enter the brain?

Lipid-soluble and non-ionic drugs Signup and view all the answers

Which route of drug administration has the highest bioavailability?

Parenteral Signup and view all the answers

Study Notes

Antidotes

Calcium Gluconate is used as an antidote for:
- Beta-Blockers (Propranolol, Sotalol)
- Calcium Channel Blockers (Verapamil)
- Diltiazem
- Isoniazid
- Hydrofluoric acid
- Anticholinergics
- Cholinergics (& vice-versa)
Other antidotes:
- Physostigmine for Anticholinergics
- Atropine for Cholinergics
- Prussian blue for Thallium
- Pyridoxine for Isoniazid

Pharmacokinetics

90% of drugs are absorbed through passive diffusion (non-ionic diffusion)
Lipid insoluble and water insoluble drugs are not absorbed from the gut
Most drugs are weakly acidic or weakly basic because stronger forms have a high ability to form corresponding ions
Protein binding:
- 0% protein binding: Lisinopril
- 99% protein binding: Oxyphenbutazone (metabolite of phenylbutazone)
- Moderate protein binding is required for efficient drug action
- Extent of binding: albumin > acid glycoprotein > lipoprotein > globulins

Bioavailability

Bioavailability of higher to lower: parenteral > oral > rectal > topical
Decreased bioavailability is due to less Vd (volume of distribution)

Pharmacodynamics

Short-acting barbiturates are due to rapid rate of distribution from brain
Only unbound drug (free form) undergoes metabolism
Unbound drug reaches liver first, then goes to other parts like kidneys
Only lipid-soluble and non-ionic drugs can enter the brain

Leukotriene Modifiers

Zafirlukast: leukotriene receptor antagonist
Zileuton: 5-lipoxygenase inhibitor, alternative therapy to low doses of inhaled steroids/nedocromil/cromolyn

Beta-Agonists

Long-acting beta2-agonists (LABA):
- Salmeterol (Serevent)
- Salmeterol with fluticasone (Advair)
Stimulate ATP-cAMP, leading to relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity

Drug Schedules

Schedule I: high abuse potential (narcotic and hallucination effects), e.g. heroin, marijuana
Schedule II: high abuse potential with severe psychic or physical dependence liability, e.g. opium, morphine, codeine

Beta-Blockers

Comparative information:
- Agents with intrinsic sympathomimetic action (ISA): Acebutolol, Carteolol, Celiprolol, Mepindolol, Oxprenolol, Pindolol
- Agents with greater aqueous solubility (hydrophilic beta blockers): Atenolol, Celiprolol, Nadolol, Sotalol
- Agents with membrane stabilizing effect: Acebutolol, Betaxolol, Pindolol, Propranolol
- Agents with antioxidant effect: Carvedilol, Nebivolol
Indication differences:
- Agents specifically indicated for cardiac arrhythmia: Esmolol, Sotalol, Landiolol
- Agents specifically indicated for congestive heart failure: Bisoprolol, Carvedilol, Sustained-release metoprolol, Nebivolol
- Agents specifically indicated for glaucoma: Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol
- Agents specifically indicated for myocardial infarction: Atenolol, Metoprolol, Propranolol
- Agents specifically indicated for migraine prophylaxis: Timolol, Propranolol
- Propranolol is the only agent indicated for control of tremor, portal hypertension, and esophageal variceal bleeding, and used in conjunction with α blocker therapy in phaeochromocytoma.

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Description

Test your knowledge on the comparative information, pharmacological differences, and indication differences of various beta blockers including agents with intrinsic sympathomimetic action, greater aqueous solubility, membrane stabilizing effect, and antioxidant effect.