Cholinergic Drugs (Parasympathetic)

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Questions and Answers

What is the primary action of Isoproterenol on the heart?

  • Increase diastolic blood pressure
  • No effect on heart rate
  • Decrease heart rate and contractility
  • Increase heart rate and contractility (correct)

Which receptor does Phenylephrine selectively act upon?

  • B2 receptor
  • a2 receptor
  • a1 receptor (correct)
  • B1 receptor

What is a caution associated with the use of Phenylephrine in elderly patients?

  • Increased risk of hypertension (correct)
  • Increased risk of hypotension
  • Increased risk of arrhythmias
  • Lowered effectiveness as a nasal decongestant

What effect does stimulation of B2 receptors have on total peripheral resistance (TPR)?

<p>Decreases total peripheral resistance (C)</p> Signup and view all the answers

Which of the following statements about selective drugs is accurate at high concentrations?

<p>They lose selectivity and affect other receptors (C)</p> Signup and view all the answers

What is the primary effect of MAO inhibitors in treating Parkinson's disease?

<p>Block metabolism of dopamine (B)</p> Signup and view all the answers

What condition may result from consuming foods high in tyramine while on MAO inhibitors?

<p>Hypertensive crisis (A)</p> Signup and view all the answers

What kind of adrenergic receptors does Ephedrine primarily act on?

<p>Non-selective alpha and beta (B)</p> Signup and view all the answers

Which effect is NOT associated with the use of alpha blockers?

<p>Increase in heart rate (C)</p> Signup and view all the answers

Which side effect is most commonly associated with the use of non-selective alpha antagonists?

<p>Postural hypotension (C)</p> Signup and view all the answers

What is the main therapeutic use of non-selective alpha antagonists like Phentolamine?

<p>For the management of hypertension during surgery (C)</p> Signup and view all the answers

How do COMT inhibitors function in regards to catecholamines?

<p>Block degradation of catecholamines (D)</p> Signup and view all the answers

Which of the following is an effect of mixed acting sympathomimetics like Ephedrine?

<p>Bronchial dilation (A)</p> Signup and view all the answers

What is a potential adverse effect of phenoxybenzamine due to its irreversible action?

<p>Chronic hypotension (B)</p> Signup and view all the answers

What mechanism does Selegiline utilize in treating depression?

<p>Blocking MAO-A metabolism (B)</p> Signup and view all the answers

What is the primary mechanism of action of artemisinin compounds in treating malaria?

<p>Generating highly reactive free radicals (C)</p> Signup and view all the answers

Which condition can result from the use of sulfadoxine in Fansidar?

<p>Steven Johnson’s syndrome (C)</p> Signup and view all the answers

Which antibiotic is commonly used in combination with quinine for treating malaria?

<p>Doxycycline (D)</p> Signup and view all the answers

What is the primary effectiveness of primaquine in malaria treatment?

<p>Radical cure and prevention of relapse (B)</p> Signup and view all the answers

What is a notable side effect of atovaquone?

<p>GI adverse effects (D)</p> Signup and view all the answers

Which drug combination is the recommended first line treatment for multidrug-resistant falciparum malaria?

<p>Artemisinin and mefloquine (D)</p> Signup and view all the answers

Which of the following statements about proguanil is true?

<p>Inhibits the enzyme dihydrofolate reductase (A)</p> Signup and view all the answers

Why is doxycycline not recommended for children?

<p>Bone and teeth deformities (A)</p> Signup and view all the answers

What stage of malaria does primaquine specifically target?

<p>Primary and latent hepatic stages (C)</p> Signup and view all the answers

Which statement about Fansidar is correct?

<p>Acts as a slow-acting blood schizonticide. (C)</p> Signup and view all the answers

What is the primary mechanism of action of Dantrolene?

<p>Interferes with calcium release from the SR (C)</p> Signup and view all the answers

Which of the following is a significant side effect of Tizanidine?

<p>Hypotension (D)</p> Signup and view all the answers

Which adrenergic receptor subtype primarily results in bronchial dilation when stimulated?

<p>b2 (C)</p> Signup and view all the answers

In which clinical situation is adrenaline primarily utilized?

<p>Cardiac arrest (A)</p> Signup and view all the answers

What effect does Noradrenaline have on heart rate?

<p>Causes reflex bradycardia (A)</p> Signup and view all the answers

What is the function of b3 adrenergic receptors?

<p>Lipolysis in adipose tissue (A)</p> Signup and view all the answers

What condition is associated with the use of Dopamine at low concentrations?

<p>Increased renal blood flow (D)</p> Signup and view all the answers

What adverse effect can be anticipated from using Dantrolene?

<p>Muscle weakness (A)</p> Signup and view all the answers

Which of the following effects is associated with alpha 1 adrenergic receptors?

<p>Vasoconstriction (C)</p> Signup and view all the answers

Which neurotransmitter is responsible for activating b1 receptors to stimulate the heart?

<p>Noradrenaline (B)</p> Signup and view all the answers

What is the primary clinical use of Dopamine?

<p>Cardiogenic shock (A)</p> Signup and view all the answers

What effect does stimulation of b2 receptors have on the uterus?

<p>Relaxation of smooth muscle (D)</p> Signup and view all the answers

Which drug binds non-selectively to all adrenergic receptors?

<p>Adrenaline (B)</p> Signup and view all the answers

In addition to treating shock, what is a common use of Noradrenaline?

<p>Septic shock (D)</p> Signup and view all the answers

Which of the following pharmacological effects is primarily associated with M2 muscarinic receptors?

<p>Inhibit neurotransmitter release (C)</p> Signup and view all the answers

What is the main therapeutic use of Methacholine?

<p>Diagnosis of bronchial hyperreactivity (C)</p> Signup and view all the answers

Which adverse effect is associated with the use of Pilocarpine?

<p>Dry mouth (A)</p> Signup and view all the answers

What is the mechanism of action of cholinesterase inhibitors?

<p>Block AChE, causing ACh accumulation (B)</p> Signup and view all the answers

Which receptor type is targeted by Nicotine as a nicotinic agonist?

<p>NN (C)</p> Signup and view all the answers

What is a significant pharmacological effect of M3 receptor activation?

<p>Miosis (B)</p> Signup and view all the answers

Which of the following is an example of a reversible acetylcholinesterase inhibitor?

<p>Edrophonium (C)</p> Signup and view all the answers

What is a primary clinical use of Acetylcholine as a drug?

<p>Surgery requiring miosis (C)</p> Signup and view all the answers

What is a characteristic of the pharmacokinetics of Acetylcholine?

<p>Rapid inactivation by cholinesterase (B)</p> Signup and view all the answers

Which type of muscarinic receptors facilitate increased gastric secretions and motility?

<p>M1 receptors (D)</p> Signup and view all the answers

What adverse effect is commonly associated with excessive stimulation of M3 receptors?

<p>Bronchoconstriction (D)</p> Signup and view all the answers

Which of the following drugs is an example of a nicotinic agonist used for skeletal muscle contraction?

<p>Suxamethonium chloride (C)</p> Signup and view all the answers

What mechanism causes the decrease in intraocular pressure (IOP) when using Pilocarpine?

<p>Increased drainage of aqueous humor (D)</p> Signup and view all the answers

Why is Acetylcholine not frequently used clinically despite its effects?

<p>Rapid inactivation and short duration (B)</p> Signup and view all the answers

What is the primary clinical use of Prazosin?

<p>Essential hypertension (B)</p> Signup and view all the answers

Which drug is preferred for the treatment of benign prostatic hyperplasia (BPH)?

<p>Tamsulosin (C)</p> Signup and view all the answers

What effect do beta blockers primarily have on the heart?

<p>Decrease heart rate (A)</p> Signup and view all the answers

Which of the following is an adverse effect of Propranolol?

<p>Bronchoconstriction (B)</p> Signup and view all the answers

What is an effect of beta-3 adrenergic receptor activation?

<p>Increased lipolysis (D)</p> Signup and view all the answers

Which medication is known to have intrinsic sympathomimetic activity (ISA)?

<p>Pindolol (B)</p> Signup and view all the answers

What action can Labetalol have during pregnancy?

<p>Decrease systemic arterial BP (C)</p> Signup and view all the answers

Which drug is specifically indicated for treating hypertension in diabetic patients?

<p>Metoprolol (C)</p> Signup and view all the answers

What condition can Chloroquine be used to treat?

<p>Malaria (D)</p> Signup and view all the answers

Yohimbine acts as a selective blocker for which adrenergic receptors?

<p>Alpha-2 (D)</p> Signup and view all the answers

Which drug is contraindicated in patients with asthma?

<p>Propranolol (C)</p> Signup and view all the answers

Which condition is Tamsulosin primarily used to treat?

<p>Benign prostatic hyperplasia (D)</p> Signup and view all the answers

What is a potential adverse effect of using Atenolol?

<p>Fatigue (C)</p> Signup and view all the answers

What is the mechanism of action of Chloroquine in treating malaria?

<p>Prevents conversion of trophozoites (A)</p> Signup and view all the answers

Flashcards

Muscarinic Agonists

A class of drugs that act as agonists at muscarinic acetylcholine receptors (mAChRs). They mimic the actions of acetylcholine in the parasympathetic nervous system.

Muscarinic Receptors

Receptors that are activated by acetylcholine in the parasympathetic nervous system and are primarily found in smooth muscles, glands, and the heart.

Muscarinic Receptor (M1)

Activation of M1 receptors in gastric parietal cells leads to increased gastric secretion and motility.

Muscarinic Receptor (M2)

Activation of M2 receptors in the heart, pre-synaptic terminals, and sphincters leads respectively to myocardial suppression, inhibition of neurotransmitter release, and sphincter relaxation.

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Muscarinic Receptor (M3)

Activation of M3 receptors in sweat glands, smooth muscles of glands and viscera of the eye leads to increased secretions, bronchoconstriction, ciliary muscle contraction and decreased intraocular pressure.

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Acetylcholinesterase (AChE)

The enzyme that breaks down acetylcholine in the synaptic cleft.

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Cholinesterase Inhibitors

Drugs that block the action of acetylcholinesterase (AChE), leading to an accumulation of acetylcholine at cholinergic synapses.

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Edrophonium

A reversible, short-acting cholinesterase inhibitor used to diagnose myasthenia gravis.

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Pilocarpine

A direct-acting, muscarinic agonist used as an ophthalmic drug for the treatment of glaucoma.

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Nicotinic Agonists

Drugs that directly stimulate nicotinic acetylcholine receptors, which are primarily found at the neuromuscular junction and in autonomic ganglia.

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Nicotine

A direct-acting, nicotinic agonist that stimulates both neuromuscular and autonomic ganglia receptors.

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Suxamethonium Chloride

A fast-acting, depolarizing muscle relaxant used for short-term paralysis.

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Nicotinic Receptor (NM)

Receptors activated by acetylcholine at the neuromuscular junction, resulting in skeletal muscle contraction.

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Nicotinic Receptor (NN)

Receptors activated by acetylcholine in autonomic ganglia, facilitating neurotransmission.

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Indirect Acting Cholinergic Agents

Drugs that mimic the actions of acetylcholine by inhibiting the breakdown of acetylcholine in the synaptic cleft.

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Selective Alpha-1 Receptor Agonist

A type of drug that selectively activates alpha-1 receptors, causing vasoconstriction, leading to increased blood pressure and other effects.

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Phenylephrine

A common example of an alpha-1 selective drug, used for nasal decongestion, treatment of rhinitis, and as a mydriatic agent.

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Isoproterenol

A direct-acting sympathomimetic drug that stimulates both beta-1 and beta-2 receptors, leading to an increase in heart rate and contractility, but also some vasodilation.

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Decrease in Total Peripheral Resistance (TPR)

A decrease in peripheral vascular resistance, which is the resistance to blood flow in the blood vessels.

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Tachycardia

A condition characterized by a rapid heart rate, often caused by excessive stimulation of beta-1 receptors.

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Direct Acting Sympathomimetics

A type of drug that directly stimulates adrenergic receptors, resulting in a variety of effects in the body.

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Adrenergic Agonist (Sympathomimetic)

A chemical messenger that activates adrenergic receptors, causing a cascading effect in the body.

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Adrenergic Receptor

A receptor that binds to adrenaline (epinephrine) and noradrenaline (norepinephrine), triggering a response within the body.

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Beta-1 Receptors (β1)

A class of receptors primarily found in the heart, kidneys, and other tissues. Stimulation of these receptors leads to increased heart rate and force of contraction.

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Beta-2 Receptors (β2)

A class of receptors found in various tissues like lungs, blood vessels, and the uterus. Their activation leads to bronchodilation, vasodilation, and relaxation of the uterus.

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Alpha-1 Receptors (α1)

A class of receptors primarily found in the vascular smooth muscles of the skin and mucous membranes, the bladder, and the iris. Their activation leads to vasoconstriction and pupil dilation.

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Alpha-2 Receptors (α2)

A class of receptors found at presynaptic nerve terminals, where they inhibit the release of neurotransmitters. They also play a role in the pancreas, inhibiting insulin release.

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Non-selective Adrenergic Agonist

An adrenergic agonist that binds non-selectively to all adrenergic receptors, causing a wide range of effects on the body.

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Adrenaline (Epinephrine)

A naturally occurring hormone and neurotransmitter, released by the adrenal glands and sympathetic nerve terminals. It binds to both alpha and beta receptors, causing varied effects in the body.

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Noradrenaline (Norepinephrine)

A neurotransmitter released from sympathetic nerve terminals. It binds to alpha and beta receptors, especially β1, causing a wide range of effects in the body.

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Dopamine

A neurotransmitter with diverse effects on the body, depending on the concentration. Low doses stimulate dopamine receptors (D1), while high doses stimulate beta-1 receptors (β1).

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Catechol-O-Methyltransferase (COMT)

An enzyme that breaks down adrenaline and noradrenaline in the body, thus regulating their duration of action.

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Monoamine Oxidase (MAO)

An enzyme involved in the breakdown of adrenaline and noradrenaline, contributing to the regulation of their effects in the body.

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Dental procedures

A clinical use of non-selective adrenergic agonists, often in a dental setting, to prolong the action of local anesthetics by causing local vasoconstriction.

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Anaphylactic Shock

A serious condition that can occur following a severe allergic reaction. Adrenaline is used as a treatment for this condition to help raise blood pressure and improve breathing.

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MAO inhibitors (MAOIs)

A class of drugs that inhibit the enzyme monoamine oxidase (MAO), responsible for breaking down neurotransmitters like dopamine, norepinephrine, and serotonin.

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MAO-B inhibitors

A type of MAOI that selectively inhibits MAO-B, an enzyme that primarily breaks down dopamine in the brain.

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COMT inhibitor

A drug that inhibits the enzyme COMT, which metabolizes catecholamines in the central nervous system (CNS) and peripheral tissues.

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Mixed acting sympathomimetics

Drugs that act on both alpha and beta adrenergic receptors, leading to a variety of effects including vasoconstriction, increased heart rate, and bronchodilation.

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Alpha blockers

Drugs that block alpha-adrenergic receptors, leading to vasodilation, decreased blood pressure, and various other effects depending on the specific receptor subtype.

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Non-selective reversible alpha blockers

A type of alpha blocker that blocks alpha-adrenergic receptors reversibly, meaning the effect is temporary.

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Non-selective irreversible alpha blockers

A type of alpha blocker that blocks alpha-adrenergic receptors irreversibly, causing a prolonged effect.

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Beta blockers

Drugs that act on beta-adrenergic receptors, leading to increased heart rate, force of contraction, and bronchodilation.

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Beta-1 selective blockers

A type of beta blocker that selectively blocks beta-1 receptors, which are primarily found in the heart.

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Non-selective beta blockers

A type of beta blocker that blocks both beta-1 and beta-2 receptors, which are found in the heart and lungs respectively.

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Artemisinin Compounds

A class of drugs used to treat malaria, known for their rapid action and effectiveness against Plasmodium falciparum, the deadliest malaria parasite.

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Prazosin

Selective alpha-1 blocker used to treat essential hypertension and benign prostatic hyperplasia (BPH).

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Artemisinin-based Combination Therapies (ACTs)

A combination therapy used for malaria treatment, consisting of an artemisinin derivative (like artesunate) and a partner drug like mefloquine or lumefantrine, which helps prevent resistance.

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Fansidar (Sulfadoxine + Pyrimethamine)

An antimalaria drug, also known as pyrimethamine/sulfadoxine, used to treat malaria caused by Plasmodium falciparum, but not for prophylaxis.

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Tamsulosin

Potent selective alpha-1 blocker preferred for treating benign prostatic hyperplasia (BPH).

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Antibiotics (Tetracycline, Doxycycline, Clindamycin)

Drugs that interfere with bacterial protein synthesis by binding to the bacterial ribosome, preventing the creation of essential proteins for bacteria to survive.

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Yohimbine

A selective alpha-2 receptor blocker that can be used for erectile dysfunction and other conditions.

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Group II Antimalarials (Proguanil, Atovaquone)

A class of drugs used against malaria, specifically targeting the erythrocytic and primary hepatic stages of the parasitic life cycle.

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Primaquine

A potent antimalaria drug used for the radical cure and prevention of relapse in vivax and ovale malaria infections.

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Propranolol

A non-selective beta blocker that acts on both beta-1 and beta-2 receptors, used for a variety of cardiovascular conditions.

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Metoprolol

A cardioselective beta blocker that primarily targets beta-1 receptors, minimizing effects on the lungs and bronchi.

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Blood Schizonticides

Antimalarial drugs that primarily target the erythrocytic stage of the parasitic life cycle, aiming to prevent the parasite from multiplying within red blood cells.

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Hemoglobinemia

A condition caused by the build-up of hemoglobin in the blood, often associated with malaria, as the parasite can damage red blood cells.

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Atenolol

A cardioselective beta blocker with minimal risk of bronchospasm, used to treat hypertension and other cardiovascular conditions.

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Pindolol

A beta blocker with intrinsic sympathomimetic activity (ISA), meaning it has some beta-agonist effects, making it suitable for patients who may experience bradycardia or bronchospasm with other beta blockers.

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Slow Acting Blood Schizonticides

A drug used to treat malaria, exhibiting a relatively slow acting mechanism and effectiveness against all forms of malaria, but it takes some time to see its full effect.

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Labetalol

A beta blocker with alpha-blocking activity, blocking both alpha-1 and beta receptors, used for hypertension and hypertensive emergencies.

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Prophylaxis

A type of treatment used to prevent malaria infection, aiming to prevent the parasite from establishing itself in the body.

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Plasmodium Falciparum

A parasite that causes malaria and is only present in blood.

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Plasmodium Vivax and Ovale

Malarial parasites that can exist in both the blood and the liver.

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Clinical Cure

Treatment of malaria that aims to relieve symptoms but does not eliminate the parasite.

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Radical Cure

Treatment of malaria aimed at completely eradicating the parasite from the body.

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Chloroquine

A common antimalarial drug that prevents the conversion of parasites to their reproductive stage.

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Study Notes

Cholinergic Drugs (Parasympathetic)

  • Cholinergic drugs mimic the parasympathetic nervous system
  • Direct-acting muscarinic agonists:
    • Increase secretions (salivation, gastric)
    • Bronchoconstriction, miosis (pupil constriction)
    • Lower intraocular pressure
    • Myocardial suppression
  • Acetylcholine:
    • Primarily controlled by inhibitory Gi-coupled M2 and excitatory Gq-coupled M3 muscarinic acetylcholine receptors (mAChRs)
    • Short duration of action
  • Methacholine:
    • Non-selective muscarinic receptor agonist
    • Increases gastric secretions, suppresses myocardial contraction
    • Used to diagnose bronchial hyperreactivity
    • Side effects: Bradycardia, hypotension, sweating, flushing
  • Pilocarpine:
    • Applied locally to eye to induce miosis, lower intraocular pressure, increase secretions
    • Used to diagnose bronchial hyperreactivity, and in surgeries requiring miosis
    • Side effects: Local irritation, blurred vision, GIT hyperreactivity
  • Direct-acting Nicotinic agonists:
    • NM (neuromuscular junction) - skeletal muscle contraction
    • NN (autonomic ganglia) - facilitate neurotransmission
    • Examples: Nicotine, Suxamethonium chloride

Indirect Acting: Cholinesterase Inhibitors

  • Inhibit acetylcholinesterase (AChE), causing acetylcholine accumulation
  • Reversible short acting: Edrophonium
    • Used to diagnose myasthenia gravis
    • Increases muscle strength
  • Reversible medium acting: Neostigmine
    • Treats myasthenia gravis, and paralytic ileus
    • Increases strength for hours
  • Reversible long acting: Physostigmine
    • Treats myasthenia gravis, glaucoma, anticholinergic poisoning
    • Longer duration of action
  • Irreversible:
    • Organophosphates (nerve gases):
      • Binds to AChE permanently
      • Causes accumulation of acetylcholine

Cholinergic Blockers

  • Inhibit the effects of acetylcholine
  • Muscarinic antagonists:
    • Atropine:
      • Reduces secretions (dry mouth)
      • Pupil dilation (mydriasis)
    • Scopolamine:
      • Motion sickness
      • Anti-cholinergic toxicity
    • Ipratropium:
      • Used in COPD
      • Side Effects: Restlessness, blurred vision, increased IOP, inhibition of sweat, dry mouth
  • Ganglion blocking agent:
    • Hexamethonium:
      • Reduces secretions
      • Causes muscle weakness and paralysis (at high doses)

Neuromuscular Blockers

  • Non-depolarizing: Tubocurarine
    • Used for endotracheal intubation and surgery
    • Competitive antagonist, preventing Ach binding
    • Blocks ACh receptors, inhibiting neuromuscular transmission
  • Depolarizing: Succinylcholine
    • Causes initial depolarization, followed by desensitization
    • Used for intubation, and muscle relaxation during surgery

Spasmolytics

  • Baclofen:
    • GABA agonist
    • Relieves excitation, relieving muscle spasms
  • Tizanidine:
    • Acts on alpha-2 receptors to reduce spasticity
    • Reducing muscle spasms and pain from multiple sclerosis

Adrenergic Agonists

  • a1 receptors:
    • Excitatory
    • Vasoconstriction, contraction, mydriasis
  • a2 receptors:
    • Inhibitory
    • Inhibition of transmitter release
  • b1 receptors:
    • Excitatory
    • Myocardial stimulation, renin secretion
  • b2 receptors:
    • Inhibitory
    • Muscle relaxation, vasodilation
  • b3 receptors:
    • Excitatory
    • Lipolysis

Adrenergic Antagonists

  • Alpha antagonists:

    • Non-selective (phenoxybenzamine, phentolamine):
      • Relaxes muscles around prostate
      • Used to diagnose and treat pheochromocytoma
    • Selective (prazosin, tamsulosin):
      • Treats benign prostatic hyperplasia (BPH)
    • Selective (Yohimbine):
  • Beta antagonists:

    • Non-selective (propranolol):
      • Treats hypertension, angina, tremor
    • Cardio-selective (metoprolol, atenolol):
      • Treats hypertension, angina
    • Intrinsic sympathomimetic activity (ISA) (pindolol, acebutolol):

Drugs for Malaria

  • Chloroquine:

    • Effective against erythrocytic stages
    • Large Vd and extensive tissue binding
    • Blocks parasite's food source
  • Quinine:

    • Treats severe and resistant P. falciparum malaria, RA
    • Higher sensitivity in CQ resistant parasites
  • Artemisinin compounds:

    • Generates highly reactive free radicals, effective against all stages
  • Sulfadoxine-pyrimethamine:

    • Effective against all stages
    • Inhibits DHPS and DHFR

Antibiotics (for Malaria, not for general infection)

  • Group II:
    • Tetracycline/doxycycline/clindamycin
    • Inhibit protein synthesis
  • Group III
    • Primaquine (Inhibits respiratory processes, effective against primary and latent hepatic stages)
    • Proguanil (Blocks parasite reproduction)
    • Atovoquone (Interferes with parasite mitochondrial function; effective against the primary liver forms)

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