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Pharm 7

front 1

The autonomic neuroeffector–junction effects of acetylcholine and similar drugs are best termed:
A. Sympatholytic effects
B. Nicotinomimetic effects
C. Adrenergic effects
D. Parasympathomimetic effects

back 1

D. Parasympathomimetic effects

front 2

A researcher classifies cholinoceptors by transmembrane signaling mechanism. Which pairing is correct?
A. Muscarinic—G protein; Nicotinic—ion channel
B. Muscarinic—ion channel; Nicotinic—G protein
C. Both are ligand-gated channels
D. Both are G protein–linked

back 2

A. Muscarinic—G protein; Nicotinic—ion channel

front 3

Which site is most consistent with muscarinic receptor localization described in autonomic pharmacology?
A. Synaptic vesicle membrane
B. Mitochondrial inner membrane
C. Effector-cell plasma membrane
D. Nuclear envelope membrane

back 3

C. Effector-cell plasma membrane

front 4

What agents bind to and activate muscarinic or nicotinic receptors?

back 4

Direct-acting

front 5

Which produce their primary effects by inhibiting acetylcholinesterase?

back 5

Indirect-acting

front 6

Acetylcholinesterase breaks Ach into?
A. Acetate and ethanol
B. Choline and acetic acid
C. Choline and propionic acid
D. Acetyl-CoA and choline

back 6

B. Choline and acetic acid

front 7

A quaternary choline ester shows minimal CNS effects even at high doses. The most direct physicochemical explanation is that it is relatively:
A. Nonpolar in plasma
B. Highly protein-bound
C. Rapidly metabolized hepatically
D. Insoluble in lipids

back 7

D. Insoluble in lipids

front 8

Two enantiomers of bethanechol are compared in vitro. One is ~1000× more potent at muscarinic receptors. Which configuration is more potent?
A. cis-bethanechol
B. trans-bethanechol
C. (S)-bethanechol
D. (R)-bethanechol

back 8

C. (S)-bethanechol

front 9

A toxicology consult notes that certain natural cholinomimetic alkaloids are well absorbed from most sites because they are tertiary amines. List them:
A. pilocarpine, nicotine, lobeline
B. pilocarpine, nicotine, muscarine
C. pilocarpine, nicotine, bethanechol
D. pilocarpine, methacholine, lobeline

back 9

A. pilocarpine, nicotine, lobeline

front 10

Several people develop cholinergic toxicity after eating wild mushrooms. Which agent is specifically noted as a quaternary amine that can still enter the brain and be toxic when ingested?
A. Carbachol
B. Methacholine
C. Muscarine
D. Bethanechol

back 10

C. Muscarine

front 11

A patient ingests a tertiary-amine cholinomimetic. Which intervention would accelerate clearance based on urinary handling?
A. Urine alkalinization
B. Forced diuresis only
C. Activated charcoal only
D. Urine acidification

back 11

D. Urine acidification

front 12

In a salivary gland acinar cell, a muscarinic agonist produces increased secretion via a classic second-messenger cascade. Which pathway is most consistent with M1/M3/M5 activation?
A. cAMP/PKA rise
B. cGMP/PKG rise
C. IP3/DAG signaling
D. JAK/STAT signaling

back 12

C. IP3/DAG signaling

front 13

In classic studies of nicotinic receptors, which tool most directly enabled receptor labeling and isolation because it binds very tightly?
A. α-bungarotoxin
B. Atropine
C. Hexamethonium
D. Physostigmine

back 13

A. α-bungarotoxin

front 14

Why were electric organs especially useful for detailed nicotinic receptor studies?
A. Minimal receptor density
B. Exclusive M3 expression
C. No ionic currents present
D. Extremely high receptor density

back 14

D. Extremely high receptor density

front 15

A patch-clamp experiment activates neuronal nicotinic receptors. Which immediate measurable change best supports successful activation as described?
A. Nuclear transcription rise
B. Ionic conductance change
C. DNA methylation shift
D. Lysosomal pH change

back 15

B. Ionic conductance change

front 16

A pharmacologist focuses on neuronal nicotinic receptors. Their subunit composition is best described as containing:
A. Only δ and ε subunits
B. α with γ only
C. α and β only
D. α with δ only

back 16

C. α and β only

front 17

A drug is desired to produce muscarinic effects with a higher likelihood of systemic absorption from multiple administration sites compared with quaternary choline esters. Which agent best fits that property?
A. Carbachol
B. Bethanechol
C. Methacholine
D. Nicotine

back 17

D. Nicotine

front 18

A resident wants a cholinomimetic with poor CNS penetration due to hydrophilicity and limited distribution. Which choice best matches?
A. Lobeline
B. Bethanechol
C. Pilocarpine
D. Nicotine

back 18

B. Bethanechol

front 19

A patient receives a cholinesterase inhibitor and develops marked muscarinic effects. The drug class responsible for the primary pharmacologic effect is best characterized as inhibiting:
A. Acetylcholinesterase
B. Choline acetyltransferase
C. Vesicular ACh transporter
D. Nicotinic receptor opening

back 19

A. Acetylcholinesterase

front 20

A patient with open-angle glaucoma receives a muscarinic agonist drop. Which ocular action most directly produces the key pupillary change?
A. Iris radial contraction
B. Ciliary muscle relaxation
C. Lens flattening
D. Iris sphincter contraction

back 20

D. Iris sphincter contraction

front 21

After the same drop, the patient can read fine print better. Which mechanism explains this near-vision effect?
A. Ciliary muscle contraction
B. Zonal fiber tightening
C. Lens flattening
D. Pupillary dilation

back 21

A. Ciliary muscle contraction

front 22

A healthy volunteer receives a minimally effective IV acetylcholine infusion (20–50 mcg/min). What pattern is most expected?
A. Hypertension with bradycardia
B. Hypertension with tachycardia
C. Hypotension with tachycardia
D. Hypotension with bradycardia

back 22

C. Hypotension with tachycardia

front 23

With larger IV acetylcholine doses, which heart-rate response becomes prominent from direct cardiac effects?
A. Bradycardia
B. Sinus tachycardia
C. Ventricular tachycardia
D. No rate change

back 23

A. Bradycardia

front 24

In isolated atrial tissue, a muscarinic agonist directly reduces the slow inward calcium current. Which current is decreased?
A. INa
B. ICa
C. IK1
D. Ito

back 24

B. ICa

front 25

A pacemaker-cell study shows slower phase 4 depolarization after a muscarinic agonist. Which current is reduced?
A. IKs
B. IKr
C. If
D. ICa

back 25

C. If

front 26

A patient has only mild net bradycardia after a muscarinic agonist despite strong direct SA slowing. Best explanation?
A. Reflex sympathetic discharge
B. SA receptor downregulation
C. Increased vagal tone
D. Direct β1 stimulation

back 26

A. Reflex sympathetic discharge

front 27

In an artery-ring lab, endothelium is mechanically removed. Which acetylcholine vascular response is most affected?
A. Increased venous tone
B. Increased arterial stiffness
C. Enhanced smooth muscle growth
D. Endothelium-dependent vasodilation

back 27

D. Endothelium-dependent vasodilation

front 28

The receptor subtype responsible for acetylcholine-induced vasodilation on intact endothelium is:
A. M1
B. M3
C. M2
D. M5

back 28

B. M3

front 29

A vasodilatory response to muscarinic stimulation depends on release of endothelium-derived relaxing factor. The mediator is:
A. Endothelin-1
B. Thromboxane A2
C. Nitric oxide
D. Histamine

back 29

C. Nitric oxide

front 30

A patient with asthma receives a systemic muscarinic agonist. Which airway effect is most likely?
A. Bronchial smooth muscle contraction
B. Bronchial smooth muscle relaxation
C. Reduced mucus secretion
D. Increased ciliary beat frequency

back 30

A. Bronchial smooth muscle contraction

front 31

After cholinomimetic exposure, a patient develops cramping and diarrhea. Which GI change best explains this?
A. Decreased motility and secretion
B. Decreased motility only
C. Increased secretion only
D. Increased motility and secretion

back 31

D. Increased motility and secretion

front 32

A muscarinic agonist is given for urinary retention. Which coordinated bladder effect promotes voiding?
A. Detrusor relaxes; sphincter contracts
B. Detrusor contracts; sphincter relaxes
C. Trigone contracts; detrusor relaxes
D. Sphincter contracts; trigone contracts

back 32

B. Detrusor contracts; sphincter relaxes

front 33

A patient on a muscarinic agonist reports watery eyes, runny nose, and heavy sweating. Which glands are directly stimulated?
A. Sebaceous glands, lacrimal, nasal
B. Apocrine sweat glands, lacrimal, nasal
C. Thermoregulatory sweat, lacrimal, nasal
D. Thyroid and parotid glands, lacrimal, nasal

back 33

C. Thermoregulatory sweat, lacrimal, nasal

front 34

A cognition study targets the muscarinic subtype richly expressed in brain regions involved in cognition. Which subtype is it?
A. M2
B. M3
C. M4
D. M1

back 34

D. M1

front 35

Despite fewer nicotinic than muscarinic receptors, nicotine and lobeline strongly affect which CNS regions?
A. Brain stem and cortex
B. Cerebellum and thalamus
C. Basal ganglia and pons
D. Spinal cord and midbrain

back 35

A. Brain stem and cortex

front 36

In hippocampal circuits, acetylcholine regulates norepinephrine release via which nicotinic receptor subtype?
A. α4β2
B. α7
C. α3β4
D. α1β1γδ

back 36

C. α3β4

front 37

A presynaptic mechanism in hippocampus and cortex limits further cholinergic signaling. What effect is described?
A. Increased acetylcholine release
B. Inhibited acetylcholine release
C. Increased norepinephrine reuptake
D. Decreased dopamine synthesis

back 37

B. Inhibited acetylcholine release

front 38

The most abundant nicotinic receptor oligomer in the brain is:
A. α3β4
B. α3
C. α7
D. α4β2

back 38

D. α4β2

front 39

Chronic nicotine exposure produces which sequence at nicotinic receptors?
A. Depolarization then desensitization
B. Desensitization then depolarization
C. Blockade then sensitization
D. Internalization then activation

back 39

A. Depolarization then desensitization

front 40

A patient ingests high-concentration nicotine and develops tremor and emesis. What additional central effect best fits?
A. Respiratory center suppression
B. Phrenic nerve blockade
C. Respiratory center stimulation
D. Central chemoreceptor inhibition

back 40

C. Respiratory center stimulation

front 41

A drug-development team targets a nicotinic subtype linked to cognition and pain perception. Which subtype matches?
A. α3
B. α7
C. α4β2
D. α3β4

back 41

B. α7

front 42

Proposed anti-inflammatory actions of α7 nicotinic receptors are based on their presence on:
A. Hepatocytes
B. Skeletal myocytes
C. Erythrocytes
D. Immune nonneuronal cells

back 42

D. Immune nonneuronal cells

front 43

Fast excitatory transmission in autonomic ganglia is primarily mediated by which nicotinic subtype?
A. α3
B. α4β2
C. α7
D. α3β4

back 43

A. α3

front 44

In autonomic ganglia and adrenal medulla, heteromeric neuronal nAChRs commonly include α3 plus:
A. β1 and β3 subunits
B. β2 only
C. β2 and β4 subunits
D. δ and ε subunits

back 44

C. β2 and β4 subunits

front 45

Compared with skeletal muscle nAChRs, nicotine has somewhat greater affinity for:
A. Neuronal nicotinic receptors
B. Muscarinic M3 receptors
C. Skeletal nicotinic receptors
D. GABA-A receptors

back 45

A. Neuronal nicotinic receptors

front 46

Which best fits deficiency? Microcystis, microcolon, and intestinal hypoperistalsis syndrome, urinary incontinence, urinary bladder distention, and mydriasis.
A. a3
B. b2
C. b4
D. m3

back 46

D. m3

front 47

A depolarizing nicotinic agonist that is not rapidly hydrolyzed causes weakness after initial activation. The transmission block most directly reflects:
A. Depolarization blockade
B. Competitive antagonism
C. Vesicular ACh depletion
D. Presynaptic Ca2+ blockade

back 47

A. Depolarization blockade

front 48

Nicotinic agonist applied to an end plate by iontophoresis causes immediate depolarization. The primary ionic basis is increased permeability to:
A. Ca2+ and Cl−
B. Na+ and K+
C. K+ and Cl−
D. Na+ and Ca2+

back 48

B. Na+ and K+

front 49

A very brief-acting cholinesterase inhibitor is used diagnostically because it is a simple alcohol with a quaternary ammonium. Which drug fits?
A. Neostigmine
B. Physostigmine
C. Echothiophate
D. Edrophonium

back 49

D. Edrophonium

front 50

Which agent is a carbamic acid ester cholinesterase inhibitor (carbamate) used clinically?
A. Neostigmine
B. Echothiophate
C. Edrophonium
D. Sarin

back 50

A. Neostigmine

front 51

Which drug is an organophosphate cholinesterase inhibitor used clinically?
A. Physostigmine
B. Neostigmine
C. Echothiophate
D. Edrophonium

back 51

C. Echothiophate

front 52

An insecticide is engineered for very high lipid solubility to speed absorption into insects and rapid CNS distribution. Which is typical?
A. Echothiophate
B. Carbaryl
C. Edrophonium
D. Physostigmine

back 52

B. Carbaryl

front 53

A clinician prefers an organophosphate with very long duration but improved stability in aqueous solution. Which agent best matches?
A. Sarin
B. Echothiophate
C. Carbaryl
D. Neostigmine

back 53

B. Echothiophate

front 54

A military exposure causes profound cholinergic crisis; the agent is an extremely potent “nerve gas.” Which is most consistent?
A. Sarin
B. Edrophonium
C. Physostigmine
D. Neostigmine

back 54

A. Sarin

front 55

A quaternary ammonium carbamate (such as Neostigmine) requires an oral dose that is significantly higher than its parenteral dose to achieve the same therapeutic effect. What is the primary pharmacokinetic reason for this difference?

A. High rates of first-pass metabolism in the liver.

B. Extensive binding to plasma albumin, reducing free drug levels

C. A permanent positive charge that limits lipid membrane permeability.

D. Rapid active secretion by the renal proximal tubules.

back 55

C. A permanent positive charge that limits lipid membrane permeability.

front 56

An AChE inhibitor is well absorbed from all sites and can be used topically in the eye. Which drug fits?
A. Neostigmine
B. Edrophonium
C. Echothiophate
D. Physostigmine

back 56

D. Physostigmine

front 57

Most organophosphate cholinesterase inhibitors are dangerous to humans because they are:
A. Poorly absorbed from skin
B. Well absorbed from mucosa
C. Selective for plasma enzymes
D. Rapidly hydrolyzed in blood

back 57

B. Well absorbed from mucosa

front 58

Which organophosphate is noted as highly polar and more stable than most others?
A. Echothiophate
B. Sarin
C. Malathion
D. Carbaryl

back 58

A. Echothiophate

front 59

You want an AChE inhibitor lasting about 5–15 minutes. Which duration matches best?
A. Physostigmine
B. Pyridostigmine
C. Edrophonium
D. Echothiophate

back 59

C. Edrophonium

front 60

A postoperative patient needs an AChE inhibitor with 0.5–4 hour action. Which agent best matches?
A. Pyridostigmine
B. Neostigmine
C. Echothiophate
D. Edrophonium

back 60

B. Neostigmine

front 61

A patient needs sustained symptomatic coverage with an AChE inhibitor lasting 4–6 hours. Which duration fits?
A. Neostigmine
B. Physostigmine
C. Echothiophate
D. Pyridostigmine

back 61

D. Pyridostigmine

front 62

A clinician selects an AChE inhibitor with 0.5–2 hour duration and good absorption from all sites. Which best fits?
A. Physostigmine
B. Edrophonium
C. Neostigmine
D. Pyridostigmine

back 62

A. Physostigmine

front 63

A glaucoma regimen uses an AChE inhibitor with ~100-hour duration. Which drug matches?
A. Neostigmine
B. Echothiophate
C. Physostigmine
D. Edrophonium

back 63

B. Echothiophate

front 64

Beyond acetylcholinesterase, these inhibitors also inhibit which enzyme?
A. Monoamine oxidase
B. Butyrylcholinesterase
C. Dopamine β-hydroxylase
D. Catechol-O-methyltransferase

back 64

B. Butyrylcholinesterase

front 65

A child with α3-subunit deficiency is evaluated. Which combination best matches the syndrome?
A. Microcolon and hyperperistalsis
B. Microcystis and microcolon
C. Megacystis and megacolon
D. Microcystis and tachycardia

back 65

B. Microcystis and microcolon

front 66

A pathologist samples adrenal medulla ganglion-like tissue. Which nAChR subunit pattern is most expected there?
A. α1β1γδ only
B. α7 only
C. α3 with β2/β4
D. α4β2 only

back 66

C. α3 with β2/β4

front 67

A new AChE inhibitor forms a covalent carbamoylated enzyme that is slowly hydrolyzed, prolonging recovery for 30 minutes to 6 hours. This mechanism best fits:
A. Quaternary alcohol inhibitors
B. Direct muscarinic agonists
C. Organophosphate nerve agents
D. Carbamate ester inhibitors

back 67

D. Carbamate ester inhibitors

front 68

Which pair are classic examples of carbamate ester AChE inhibitors?
A. Edrophonium and atropine
B. Neostigmine and physostigmine
C. Echothiophate and sarin
D. Pilocarpine and cevimeline

back 68

B. Neostigmine and physostigmine

front 69

The most prominent pharmacologic effects of cholinesterase inhibitors are most evident in:
A. CV, GI, eye, NMJ
B. Liver, kidney, spleen, bone
C. Thyroid, pancreas, testes, skin
D. Lung, pleura, marrow, lymph

back 69

A. CV, GI, eye, NMJ

front 70

A lipid-soluble AChE inhibitor at low concentration produces diffuse EEG activation and subjective alertness. This effect most directly reflects:
A. Neuromuscular transmission failure
B. Primary vascular smooth muscle action
C. Peripheral muscarinic blockade
D. Central cholinergic stimulation

back 70

D. Central cholinergic stimulation

front 71

At high concentrations, lipid-soluble AChE inhibitors can cause generalized convulsions followed by coma and:
A. Severe hyperthermia
B. Respiratory arrest
C. Acute hepatic necrosis
D. Ventricular fibrillation

back 71

B. Respiratory arrest

front 72

A patient exposed to an AChE inhibitor shows increased autonomic outflow. These drugs can increase activity in:
A. Only parasympathetic ganglia
B. Only sympathetic ganglia
C. Both sympathetic and parasympathetic
D. Only postganglionic terminals

back 72

C. Both sympathetic and parasympathetic

front 73

Edrophonium, neostigmine, and physostigmine most closely mimic which physiologic input on the heart?
A. Renin-angiotensin activation
B. Carotid body stimulation
C. Cardiac β1 stimulation
D. Vagal nerve activation

back 73

D. Vagal nerve activation

front 74

Cholinesterase inhibitors have minimal effects by direct action on vascular smooth muscle because:
A. Most beds lack cholinergic innervation
B. Vascular AChE is absent
C. Vascular muscle lacks muscarinic receptors
D. Blood vessels lack smooth muscle

back 74

A. Most beds lack cholinergic innervation

front 75

Moderate doses of AChE inhibitors can raise blood pressure primarily by increasing systemic:
A. Venous capacitance
B. Stroke volume
C. Vascular resistance
D. Plasma volume

back 75

C. Vascular resistance

front 76

In quaternary nitrogen AChE inhibitors, the pressor response is initiated mainly at:
A. Carotid baroreceptors
B. Sympathetic ganglia
C. Ventricular myocardium
D. Renal juxtaglomerular cells

back 76

B. Sympathetic ganglia

front 77

In lipid-soluble AChE inhibitors, the pressor response can also be initiated at:
A. Central sympathetic centers
B. Ventral horn motor neurons
C. Endothelial M3 receptors
D. AV nodal pacemakers

back 77

A. Central sympathetic centers

front 78

A patient given an AChE inhibitor develops increased BP and plasma norepinephrine; atropine prevents both. This best implies atropine acts:
A. At NMJ
B. At endothelium
C. At parasympathetic ganglia
D. In central and peripheral sites

back 78

D. In central and peripheral sites

front 79

A patient has weakness after a curare-like blocker. An AChE inhibitor improves strength mainly by increasing:
A. Contraction strength at NMJ
B. Myosin ATPase activity
C. Calcium release from SR
D. Sodium channel inactivation

back 79

A. Contraction strength at NMJ

front 80

A key clinical use category of cholinomimetics is treatment of:
A. Essential hypertension
B. Hyperthyroidism
C. Bacterial meningitis
D. Alzheimer’s disease

back 80

D. Alzheimer’s disease

front 81

Muscarinic stimulants and AChE inhibitors reduce intraocular pressure chiefly by:
A. Iris radial contraction
B. Decreased episcleral venous pressure
C. Ciliary body contraction
D. Increased aqueous production

back 81

C. Ciliary body contraction

front 82

In depressed smooth muscle activity without obstruction, cholinomimetics may be helpful. Before use, the clinician must exclude:
A. Hypovolemia
B. Mechanical obstruction
C. Fever
D. Hypercalcemia

back 82

B. Mechanical obstruction

front 83

Among choline ester cholinomimetics, the most widely used for GI/GU disorders is:
A. Acetylcholine
B. Bethanechol
C. Carbachol
D. Methacholine

back 83

B. Bethanechol

front 84

A patient with chronic xerostomia is treated with a long-used agent to increase salivary secretion. Which fits?
A. Pilocarpine
B. Echothiophate
C. Pyridostigmine
D. Atropine

back 84

A. Pilocarpine

front 85

A patient with Sjögren syndrome and dry mouth is started on a newer direct-acting muscarinic agonist. Which drug is intended?
A. Physostigmine
B. Cevimeline
C. Neostigmine
D. Edrophonium

back 85

B. Cevimeline

front 86

In myasthenia gravis, antibodies target the main immunogenic region on which nicotinic receptor subunit?

back 86

α1

front 87

One MG mechanism reduces receptor number, accelerating internalization and degradation. This is best described as:
A. Complement inhibition
B. Presynaptic blockade
C. Receptor cross-linking
D. Vesicular depletion

back 87

C. Receptor cross-linking

front 88

Another MG mechanism reduces transmission when antibodies bind the receptor and:
A. Inhibit receptor function
B. Increase ACh release
C. Enhance channel opening
D. Activate G proteins

back 88

A. Inhibit receptor function

front 89

A patient with generalized MG remains weak despite optimized pyridostigmine. Which adjunct is most appropriate for more widespread weakness?
A. Immunosuppressant therapy
B. Chronic β-agonist therapy
C. High-dose atropine daily
D. Long-term organophosphate

back 89

A. Immunosuppressant therapy

front 90

Following edrophonium in true MG, improvement in strength typically lasts about:
A. 30 seconds
B. 30 minutes
C. 2 hours
D. 5 minutes

back 90

D. 5 minutes

front 91

Long-term symptomatic therapy for MG is most commonly maintained with:
A. Tacrine
B. Donepezil
C. Pyridostigmine
D. Echothiophate

back 91

C. Pyridostigmine

front 92

If pyridostigmine cannot be used for MG maintenance, the classic alternative is:
A. Neostigmine
B. Physostigmine
C. Edrophonium
D. Galantamine

back 92

A. Neostigmine

front 93

Because AChE inhibitors are short-acting, pyridostigmine often requires dosing about every:
A. 2 hours
B. 4 hours
C. 6 hours
D. 12 hours

back 93

C. 6 hours

front 94

Neostigmine often requires dosing about every:
A. 4 hours
B. 6 hours
C. 8 hours
D. 24 hours

back 94

A. 4 hours

front 95

After surgery, rapid reversal of nondepolarizing neuromuscular blockade is commonly accomplished with:
A. Neostigmine or edrophonium
B. Tacrine or donepezil
C. Pilocarpine or cevimeline
D. Atropine or scopolamine

back 95

A. Neostigmine or edrophonium

front 96

Which toxidrome is potentially lethal in children and can cause prolonged behavioral disturbance and arrhythmias in adults?
A. Nicotine intoxication
B. Atropine intoxication
C. Cholinergic crisis
D. Opioid intoxication

back 96

B. Atropine intoxication

front 97

A suicidal ingestion causes severe muscarinic blockade and QRS widening risk. Which drug class is classically implicated?
A. SSRIs
B. Tricyclic antidepressants
C. MAO inhibitors
D. Antipsychotics

back 97

B. Tricyclic antidepressants

front 98

The first drug used for mild-to-moderate Alzheimer’s disease with anticholinesterase and other cholinomimetic actions was:
A. Tacrine
B. Rivastigmine
C. Galantamine
D. Donepezil

back 98

A. Tacrine

front 99

Which set are newer, more selective AChE inhibitors with similar marginal benefit but less toxicity than tacrine?
A. Donepezil, galantamine, rivastigmine
B. Neostigmine, edrophonium, physostigmine
C. Pilocarpine, cevimeline, bethanechol
D. Atropine, scopolamine, ipratropium

back 99

A. Donepezil, galantamine, rivastigmine

front 100

Overdose of pilocarpine or choline esters most predictably causes:
A. Muscarinic excess signs
B. Pure nicotinic blockade
C. Isolated CNS depression
D. α-adrenergic activation

back 100

A. Muscarinic excess signs

front 101

Which symptom set best matches muscarinic excess from cholinomimetic overdose?
A. Urinary urgency and sweating
B. Mydriasis and dry skin
C. Constipation and tachycardia
D. Hyperthermia and delirium

back 101

A. Urinary urgency and sweating

front 102

The most dangerous toxic effect of large nicotine doses includes central stimulation causing:
A. Hyporeflexia
B. Convulsions
C. Catatonia
D. Miosis

back 102

B. Convulsions

front 103

Another dangerous nicotine toxicity mechanism is end-plate:
A. Hyperpolarization
B. Depolarization
C. Demyelination
D. Calcium depletion

back 103

B. Depolarization

front 104

Severe nicotine toxicity can also produce hypertension with cardiac:
A. Asystole only
B. Arrhythmias
C. Tamponade
D. Pericarditis

back 104

B. Arrhythmias

front 105

The primary neurotransmitter of the parasympathetic nervous system is:
A. Dopamine
B. Norepinephrine
C. Acetylcholine
D. Serotonin

back 105

C. Acetylcholine

front 106

Muscarinic receptors are GPCRs with how many transmembrane domains?

back 106

7

front 107

The muscarinic receptor domain classically coupled to G proteins is the:
A. 1st extracellular loop
B. 2nd extracellular loop
C. 2nd cytoplasmic loop
D. 3rd cytoplasmic loop

back 107

D. 3rd cytoplasmic loop

front 108

Nicotinic receptors are primarily found in which set of locations?
A. Autonomic ganglia, skeletal NMJ, adrenal
B. Thyroid, liver, kidney
C. Retina, cochlea, lens
D. Spleen, pancreas, marrow

back 108

A. Autonomic ganglia, skeletal NMJ, adrenal

front 109

M1 receptor—best matching location, G protein, and pathway:
A. Heart; Gi; ↓cAMP
B. CNS/nerves; Gq; IP3/DAG
C. Smooth muscle; Gi; ↓cAMP
D. Glands; Gs; ↑cAMP

back 109

B. CNS/nerves; Gq; IP3/DAG

front 110

M2 receptor—best matching location, G protein, and pathway:
A. Heart nodes; Gi; ↓cAMP
B. CNS; Gq; IP3/DAG
C. Smooth muscle; Gq; IP3/DAG
D. Glands; Gi; ↓cAMP

back 110

A. Heart nodes; Gi; ↓cAMP

front 111

M3 receptor—best matching location, G protein, and pathway:
A. Heart; Gi; ↓cAMP
B. CNS; Gi; ↓cAMP
C. Smooth muscle/glands; Gq; IP3/DAG
D. Skeletal NMJ; ion channel

back 111

C. Smooth muscle/glands; Gq; IP3/DAG

front 112

M4 and M5 are CNS receptors. Which pairing is correct?
A. M4: Gq/IP3; M5: Gi/↓cAMP
B. M4: Gi/↓cAMP; M5: Gq/IP3
C. M4: Gs/↑cAMP; M5: Gi/↓cAMP
D. M4: ion channel; M5: Gq/IP3

back 112

B. M4: Gi/↓cAMP; M5: Gq/IP3

front 113

In a healthy artery with intact endothelium, acetylcholine activates M3 receptors. Net vascular effect is:
A. Vasoconstriction via Ca2+ influx
B. No change in vascular tone
C. Vasodilation via NO release
D. Vasoconstriction via endothelin

back 113

C. Vasodilation via NO release

front 114

The key smooth-muscle second messenger that mediates NO-driven relaxation is:
A. cGMP
B. IP3
C. cAMP
D. DAG

back 114

A. cGMP

front 115

In an endothelium-denuded vessel ring, acetylcholine most likely causes:
A. Vasodilation via prostacyclin
B. Vasodilation via NO
C. No response without endothelium
D. Vasoconstriction via IP3-Ca2+

back 115

D. Vasoconstriction via IP3-Ca2+

front 116

A direct-acting cholinomimetic produces effects primarily by:
A. Blocking vesicular ACh uptake
B. Activating M or N receptors
C. Inhibiting COMT
D. Stimulating NE release

back 116

B. Activating M or N receptors

front 117

Butyrylcholinesterase inhibition matters clinically because it can act as a:
A. Cardiac pacemaker stabilizer
B. Muscarinic receptor chaperone
C. Nicotinic channel pore blocker
D. Biological scavenger enzyme

back 117

D. Biological scavenger enzyme

front 118

Which list contains only choline ester direct agonists?
A. Nicotine, muscarine, lobeline, pilocarpine
B. ACh, methacholine, carbachol, bethanechol
C. Neostigmine, pyridostigmine, edrophonium, physostigmine
D. Atropine, scopolamine, ipratropium, tiotropium

back 118

B. ACh, methacholine, carbachol, bethanechol

front 119

Choline ester lipid insolubility is mainly due to:
A. Multiple aromatic rings
B. High molecular weight
C. Sulfhydryl side chains
D. Quaternary ammonium charge

back 119

D. Quaternary ammonium charge

front 120

Which list contains only alkaloid direct agonists?
A. ACh, methacholine, carbachol, bethanechol
B. Neostigmine, physostigmine, echothiophate, edrophonium
C. Muscarine, pilocarpine, nicotine, lobeline
D. Atropine, scopolamine, tiotropium, ipratropium

back 120

C. Muscarine, pilocarpine, nicotine, lobeline

front 121

Which agent reliably activates both muscarinic and nicotinic receptors?
A. Carbachol
B. Bethanechol
C. Pilocarpine
D. Muscarine

back 121

A. Carbachol

front 122

Neonicotinoid insecticides act primarily at:
A. Muscarinic receptors
B. GABA-A receptors
C. Nicotinic receptors
D. Dopamine receptors

back 122

C. Nicotinic receptors

front 123

In the PLC pathway, DAG primarily:
A. Releases Ca2+ from SR
B. Inhibits adenylate cyclase
C. Activates guanylyl cyclase
D. Activates protein kinase C

back 123

D. Activates protein kinase C

front 124

In the PLC pathway, IP3 primarily:
A. Opens Na+ channels
B. Releases Ca2+ from stores
C. Inhibits phosphodiesterase
D. Activates PKC directly

back 124

B. Releases Ca2+ from stores

front 125

M2 and M4 receptor signaling most directly:
A. Activates PLC
B. Activates tyrosine kinase
C. Inhibits adenylate cyclase
D. Opens NMJ Na+ channels

back 125

C. Inhibits adenylate cyclase

front 126

In cardiac tissue, muscarinic stimulation most characteristically:
A. Increases K+ flux
B. Decreases K+ flux
C. Increases Na+ flux
D. Decreases Cl− flux

back 126

A. Increases K+ flux

front 127

In autonomic ganglia and many smooth muscles, muscarinic stimulation tends to:
A. Increase K+ efflux
B. Increase K+ influx
C. Increase Ca2+ influx
D. Decrease K+ flux

back 127

D. Decrease K+ flux

front 128

With nicotinic receptors, binding both agonist sites:
A. Closes the channel rapidly
B. Prevents ion selectivity
C. Lowers opening probability
D. Greatly increases opening probability

back 128

D. Greatly increases opening probability

front 129

Binding only one nicotinic site typically:
A. Abolishes channel opening
B. Forces full channel opening
C. Increases opening probability
D. Converts receptor to GPCR

back 129

C. Increases opening probability

front 130

A glaucoma drop causes miosis and accommodation. These changes:
A. Reduce Schlemm canal flow
B. Increase aqueous outflow
C. Increase aqueous production
D. Block trabecular drainage

back 130

B. Increase aqueous outflow

front 131

The aqueous humor drainage structure most directly facilitated is the:
A. Canal of Schlemm
B. Ciliary processes
C. Vitreous chamber
D. Choroid plexus

back 131

A. Canal of Schlemm

front 132

A muscarinic agonist slows the SA node primarily by:
A. Increasing conduction velocity
B. Decreasing firing rate
C. Increasing contractile force
D. Shortening refractoriness

back 132

B. Decreasing firing rate

front 133

At the AV node, muscarinic activation most characteristically:
A. Increases conduction velocity
B. Shortens refractory period
C. Slows conduction; ↑ refractory
D. Triggers ventricular ectopy

back 133

C. Slows conduction; ↑ refractory

front 134

In the atria, muscarinic stimulation most characteristically:
A. Decreases strength; ↓ refractory
B. Increases force; ↓ refractory
C. Decreases force; ↑ refractory
D. Increases force; ↑ refractory

back 134

A. Decreases strength; ↓ refractory

front 135

In the ventricles, muscarinic stimulation produces a:
A. Large force increase
B. Small strength decrease
C. Large force decrease
D. No change in force

back 135

B. Small strength decrease

front 136

Muscarinic slowing of diastolic depolarization includes reducing:
A. Hyperpolarization-activated current
B. Rapid Na current
C. Transient outward K current
D. L-type Ca current

back 136

A. Hyperpolarization-activated current

front 137

Without intact endothelium, ACh can constrict vessels because M3 on VSM triggers:
A. cGMP fall with relaxation
B. IP3-mediated Ca2+ rise
C. cAMP rise with relaxation
D. β2-mediated hyperpolarization

back 137

B. IP3-mediated Ca2+ rise

front 138

A systemic muscarinic agonist most predictably causes:
A. Bronchoconstriction
B. Bronchodilation
C. Reduced airway mucus
D. Increased dead-space ventilation

back 138

A. Bronchoconstriction

front 139

Typical GI effects of muscarinic stimulation include:
A. ↓ peristalsis; ↑ sphincters
B. ↑ peristalsis; ↑ sphincters
C. ↑ peristalsis; ↓ sphincters
D. ↓ secretion; ↑ sphincters

back 139

C. ↑ peristalsis; ↓ sphincters

front 140

Choline esters are well/poorly absorbed and distributed in the CNS

back 140

poorly

front 141

Relative abundance is best summarized as:
A. Brain muscarinic; spinal nicotinic
B. Brain nicotinic; spinal muscarinic
C. Brain muscarinic; spinal muscarinic
D. Brain nicotinic; spinal nicotinic

back 141

A. Brain muscarinic; spinal nicotinic

front 142

M1 knockout is associated with:
A. Increased appetite and obesity
B. Severe neuromuscular paralysis
C. Impaired forebrain plasticity
D. Loss of spinal pain reflexes

back 142

C. Impaired forebrain plasticity

front 143

M2 knockout is associated with:

A. Increased appetite and obesity
B. Severe neuromuscular paralysis
C. Impaired forebrain plasticity
D. Tremor and lack of pain

back 143

D. Tremor and lack of pain

front 144

Hypothalamic M3 receptor knockout is associated with:
A. Increased body fat mass
B. Increased appetite signals
C. Hyperphagia with obesity
D. Reduced appetite and fat

back 144

D. Reduced appetite and fat

front 145

Regarding autonomic ganglia, nicotine’s action on sympathetic vs parasympathetic is:
A. Same direction in both
B. Opposite direction in both
C. Only parasympathetic affected
D. Only sympathetic affected

back 145

A. Same direction in both

front 146

Nicotine’s cardiovascular effects are best described as:
A. Parasympathomimetic
B. Sympathomimetic
C. Purely muscarinic
D. Purely ganglionic block

back 146

B. Sympathomimetic

front 147

Nicotine’s GI and urinary effects are best described as:
A. Sympathomimetic
B. Antimuscarinic
C. Parasympathomimetic
D. Purely nicotinic blockade

back 147

C. Parasympathomimetic

front 148

Which agent is muscarinic-selective and a choline ester?
A. Carbachol
B. Nicotine
C. Lobeline
D. Bethanechol

back 148

D. Bethanechol

front 149

A pharmacology exam asks for two carbamate indirect-acting cholinomimetics. Which pair is correct?
A. Edrophonium, pyridostigmine
B. Neostigmine, physostigmine
C. Echothiophate, sarin
D. Pilocarpine, bethanechol

back 149

B. Neostigmine, physostigmine

front 150

A farmer presents after insecticide exposure; you suspect an organophosphate. Which set contains only organophosphate examples from your notes?
A. Echothiophate, sarin, malathion
B. Neostigmine, sarin, bethanechol
C. Edrophonium, physostigmine, sarin
D. Pilocarpine, parathion, neostigmine

back 150

A. Echothiophate, sarin, malathion

front 151

Parathion and malathion are best characterized as:
A. Active phosphates in humans
B. Quaternary carbamate salts
C. Thiophosphate prodrugs
D. Direct muscarinic agonists

back 151

C. Thiophosphate prodrugs

front 152

You need a very short-acting alcohol AChE inhibitor for bedside testing. Best choice?
A. Edrophonium
B. Neostigmine
C. Physostigmine
D. Echothiophate

back 152

A. Edrophonium

front 153

Which class is generally better absorbed and therefore more dangerous to humans (and effective insecticides)?
A. Quaternary alcohols
B. Carbamates
C. Choline esters
D. Organophosphates

back 153

D. Organophosphates

front 154

Which group typically has poor absorption because of permanent charge, requiring larger oral doses?
A. Lipid-soluble organophosphates
B. Quaternary carbamates
C. Thiophosphate nerve gases
D. Tertiary AChE inhibitors

back 154

B. Quaternary carbamates

front 155

The functional result of carbamate/organophosphate AChE inhibition is best summarized as:
A. Increased choline uptake
B. Increased ACh synthesis
C. Direct receptor antagonism
D. Blocked ACh hydrolysis

back 155

D. Blocked ACh hydrolysis

front 156

Rank duration (longest → shortest): edrophonium, carbamates, organophosphates.
A. Carbamates > edrophonium > organophosphates
B. Organophosphates > carbamates > edrophonium
C. Edrophonium > organophosphates > carbamates
D. Organophosphates > edrophonium > carbamates

back 156

B. Organophosphates > carbamates > edrophonium

front 157

A student asks what is most prescribed now for chronic glaucoma (instead of cholinomimetics). Best answer?
A. Pilocarpine plus neostigmine
B. Atropine plus timolol
C. PG analogs and topical β-blockers
D. Methacholine and acetazolamide

back 157

C. PG analogs and topical β-blockers

front 158

Acute angle-closure glaucoma is a medical emergency. Initial medical therapy commonly includes:
A. Pilocarpine
B. Donepezil
C. Atropine
D. Varenicline

back 158

A. Pilocarpine

front 159

A 5-year-old with hyperopia develops strabismus triggered by focusing effort. This fits:
A. Convergence spasm
B. Accommodative esotropia
C. CN VI palsy
D. Internuclear ophthalmoplegia

back 159

B. Accommodative esotropia

front 160

Bethanechol’s clinical profile is best described as:
A. Increases GI/GU motility, secretions
B. Selective nicotinic ganglionic blocker
C. CNS-only acetylcholinesterase inhibitor
D. Long-acting organophosphate insecticide

back 160

A. Increases GI/GU motility, secretions

front 161

Another MG mechanism reduces transmission via:
A. Terminal sprouting failure
B. Reduced ACh synthesis
C. Postsynaptic membrane lysis
D. Increased ACh breakdown

back 161

C. Postsynaptic membrane lysis

front 162

MG antibodies can also bind the receptor and:
A. Increase channel open time
B. Inhibit receptor function
C. Enhance ACh release
D. Activate G proteins

back 162

B. Inhibit receptor function

front 163

A patient has ptosis and fatigable proximal weakness. Which bedside diagnostic drug is used IV?
A. Pyridostigmine
B. Bethanechol
C. Donepezil
D. Edrophonium

back 163

D. Edrophonium

front 164

MG patients are notably sensitive to which agents during anesthesia?
A. Curariform blockers
B. β-agonists
C. Nitrates
D. Acetazolamide

back 164

A. Curariform blockers

front 165

A nondepolarizing neuromuscular relaxant listed as an anesthesia adjunct is:
A. Pancuronium
B. Succinylcholine
C. Lidocaine
D. Diazepam

back 165

A. Pancuronium

front 166

Immediate reversal of pharmacologic nondepolarizing paralysis post-op commonly uses:
A. Donepezil and rivastigmine
B. Pilocarpine and bethanechol
C. Neostigmine and edrophonium
D. Malathion and parathion

back 166

C. Neostigmine and edrophonium

front 167

Which finding is least consistent with classic AChE inhibitor toxicity (DUMBBELS)?
A. Bronchospasm
B. Lacrimation
C. Bradycardia
D. Mydriasis

back 167

D. Mydriasis

front 168

Flaccid paralysis in severe AChE inhibitor poisoning is most directly due to:
A. NMJ AChR overactivation
B. Direct myosin inhibition
C. Na+ channel blockade
D. NMJ receptor destruction

back 168

A. NMJ AChR overactivation

front 169

A patient eats Inocybe mushrooms and develops salivation, diarrhea, bronchospasm. Best antidote?
A. Pralidoxime
B. Physostigmine
C. Atropine
D. Neostigmine

back 169

C. Atropine

front 170

Nicotine replacement with varenicline works because it is a partial agonist at:
A. α7 nAChR
B. α4β2 nAChR
C. M2 receptor
D. GABA-A receptor

back 170

B. α4β2 nAChR

front 171

Varenicline reduces nicotine reinforcement mainly by reducing presynaptic:
A. GABA release
B. Serotonin release
C. NE reuptake
D. Dopamine release

back 171

D. Dopamine release

front 172

The major cause of acute cholinergic toxicity worldwide is exposure to:
A. Organophosphate insecticides
B. Tricyclic antidepressants
C. Belladonna alkaloids
D. Antihistamines

back 172

A. Organophosphate insecticides

front 173

If given quickly, nucleophiles like _______ can be used as cholinesterase regenerators for organophosphate poisoning?
A. Donepezil
B. Atropine
C. Pralidoxime
D. Pilocarpine

back 173

C. Pralidoxime

front 174

In organophosphate poisoning, which drug reverses central and peripheral muscarinic toxicity but not flaccid paralysis?
A. Pralidoxime
B. Atropine
C. Pyridostigmine
D. Rivastigmine

back 174

B. Atropine

front 175

Chronic cholinesterase inhibitor exposure can cause delayed neuropathy via NTE inhibition. Prototype agent?
A. Malathion
B. Echothiophate
C. Sarin
D. Triorthocresyl phosphate

back 175

D. Triorthocresyl phosphate

front 176

Which cholinomimetic is used for asthma challenge testing due to bronchoconstriction?
A. Bethanechol
B. Methacholine
C. Pilocarpine
D. Varenicline

back 176

B. Methacholine

front 177

Varenicline use may be limited by which adverse-effect cluster?
A. Nephrolithiasis, rash, anemia
B. Hypotension, bradycardia, syncope
C. Hepatitis, pancreatitis, arrhythmia
D. Nausea, insomnia, psychiatric worsening

back 177

D. Nausea, insomnia, psychiatric worsening

front 178

Typical severe organophosphate poisoning progression is best described as:
A. Nicotinic → CNS → muscarinic
B. Muscarinic → CNS → nicotinic
C. CNS → muscarinic → nicotinic
D. CNS → nicotinic → muscarinic

back 178

B. Muscarinic → CNS → nicotinic

front 179

Pralidoxime’s limitation in organophosphate poisoning is that it:
A. Cannot enter CNS
B. Worsens bronchospasm
C. Blocks nicotinic receptors
D. Causes irreversible AChE inhibition

back 179

A. Cannot enter CNS

front 180

Parathion and malathion insecticides are “inactive” because they require conversion to:
A. Carbamate derivatives
B. Quaternary alcohols
C. Phosphate derivatives
D. Muscarinic antagonists

back 180

C. Phosphate derivatives

front 181

Muscarinic agonists for use in the eye must be tailored to which muscarinic receptor?

back 181

M3

front 182

No improvement in a patient's condition after administration of edrophonium is indicative that the patient is undergoing (myasthenic/cholinergic) crisis

back 182

cholinergic

front 183

A marked improvement in one's condition after the administration of edrophonium is indicative of the patient undergoing (myasthenic/cholinergic) crisis

back 183

myasthenic

front 184

True or False: Amifampridine is indicated for MG?

back 184

False. Lambert-Eaton myasthenic syndrome