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Questions and Answers
Which side effect is specifically mentioned as being diminished with regular use of cholinergic antagonists?
Which side effect is specifically mentioned as being diminished with regular use of cholinergic antagonists?
- Blurred vision (correct)
- Constipation
- Confusion
- Dry mouth
What is the neurochemical effect of nicotine at low doses?
What is the neurochemical effect of nicotine at low doses?
- Increases peristalsis
- Decreases blood pressure (correct)
- Increases heart rate
- Increases secretions
Which drug is a non-depolarizing skeletal neuromuscular junction blocker?
Which drug is a non-depolarizing skeletal neuromuscular junction blocker?
- Curare
- Succinylcholine
- Aminoglycosides
- Vecuronium (correct)
What is the therapeutic use of curare (d-Tubocurarine)?
What is the therapeutic use of curare (d-Tubocurarine)?
Which drug interaction inhibits acetylcholine release from the neuromuscular junction, potentiating the effect of blockers?
Which drug interaction inhibits acetylcholine release from the neuromuscular junction, potentiating the effect of blockers?
What does succinylcholine attach to when exerting its action?
What does succinylcholine attach to when exerting its action?
Which adverse effect is NOT commonly associated with cholinergic antagonist atropine?
Which adverse effect is NOT commonly associated with cholinergic antagonist atropine?
What is the primary therapeutic use of ipratropium and tiotropium?
What is the primary therapeutic use of ipratropium and tiotropium?
Which medication is NOT a synthetic atropine-like drug used in the treatment of an overreactive bladder?
Which medication is NOT a synthetic atropine-like drug used in the treatment of an overreactive bladder?
What is the primary action of scopolamine in addition to being a belladonna alkaloid like atropine?
What is the primary action of scopolamine in addition to being a belladonna alkaloid like atropine?
Which of the following is a common pharmacokinetic characteristic of cholinergic antagonist medications like atropine?
Which of the following is a common pharmacokinetic characteristic of cholinergic antagonist medications like atropine?
What is the primary therapeutic use of tropicamide and cyclopentolate?
What is the primary therapeutic use of tropicamide and cyclopentolate?
What is the primary mechanism of action of succinylcholine?
What is the primary mechanism of action of succinylcholine?
What is the therapeutic use of succinylcholine?
What is the therapeutic use of succinylcholine?
Which adverse effect can result from using succinylcholine in conjunction with halothane?
Which adverse effect can result from using succinylcholine in conjunction with halothane?
What is the primary mechanism of action of baclofen?
What is the primary mechanism of action of baclofen?
How does dantrolene exert its effect on skeletal muscles?
How does dantrolene exert its effect on skeletal muscles?
What is the primary mechanism of action of orphenadrine for causing analgesia and muscle relaxation?
What is the primary mechanism of action of orphenadrine for causing analgesia and muscle relaxation?
How does nicotine affect the autonomic nervous system and striated muscle at a low dose?
How does nicotine affect the autonomic nervous system and striated muscle at a low dose?
Which cholinergic antagonist is specifically effective in treating organophosphate intoxication?
Which cholinergic antagonist is specifically effective in treating organophosphate intoxication?
What is the primary therapeutic use of curare (d-Tubocurarine)?
What is the primary therapeutic use of curare (d-Tubocurarine)?
What is the primary effect of scopolamine, a belladonna alkaloid similar to atropine but with a longer action in the CNS?
What is the primary effect of scopolamine, a belladonna alkaloid similar to atropine but with a longer action in the CNS?
At high doses, what is the action of Curare (d-Tubocurarine) at the skeletal neuromuscular junction?
At high doses, what is the action of Curare (d-Tubocurarine) at the skeletal neuromuscular junction?
What is the synthetic atropine-like medication used in the treatment of overactive bladder?
What is the synthetic atropine-like medication used in the treatment of overactive bladder?
Which drug interaction potentiates the effect of blockers like tebocurarine and other competitive blockers in neuromuscular blockade?
Which drug interaction potentiates the effect of blockers like tebocurarine and other competitive blockers in neuromuscular blockade?
Which centrally acting antimuscarinic agent is primarily employed as an adjuvant therapy in Parkinson's Disease?
Which centrally acting antimuscarinic agent is primarily employed as an adjuvant therapy in Parkinson's Disease?
What is the last muscle affected by muscle paralysis caused by Curare (d-Tubocurarine)?
What is the last muscle affected by muscle paralysis caused by Curare (d-Tubocurarine)?
What is the primary pharmacokinetic characteristic of cholinergic antagonist medications like atropine?
What is the primary pharmacokinetic characteristic of cholinergic antagonist medications like atropine?
Which type of neuromuscular blocker attaches to nicotinic receptors acting like acetylcholine?
Which type of neuromuscular blocker attaches to nicotinic receptors acting like acetylcholine?
Which cholinergic antagonist is NOT commonly associated with blurred vision as an adverse effect?
Which cholinergic antagonist is NOT commonly associated with blurred vision as an adverse effect?
Which drug binds to GABAB receptors and causes hyperpolarization of the neuronal membrane?
Which drug binds to GABAB receptors and causes hyperpolarization of the neuronal membrane?
What is the primary mechanism of action of dantrolene in inhibiting muscle contractions?
What is the primary mechanism of action of dantrolene in inhibiting muscle contractions?
Which adverse effect can occur when succinylcholine is used in genetically deficient patients of plasma cholinesterase?
Which adverse effect can occur when succinylcholine is used in genetically deficient patients of plasma cholinesterase?
What is the primary therapeutic use of diazepam (Valium)?
What is the primary therapeutic use of diazepam (Valium)?
How does baclofen exert its muscle relaxant effect?
How does baclofen exert its muscle relaxant effect?
Which drug, when used with halothane, may lead to malignant hyperthermia in genetically susceptible individuals?
Which drug, when used with halothane, may lead to malignant hyperthermia in genetically susceptible individuals?
Which drug, when used with halothane, may lead to malignant hyperthermia in genetically susceptible individuals?
Which drug, when used with halothane, may lead to malignant hyperthermia in genetically susceptible individuals?
Which of the following drugs binds to GABAB receptors leading to hyperpolarization of the neuronal membrane?
Which of the following drugs binds to GABAB receptors leading to hyperpolarization of the neuronal membrane?
What is the primary adverse effect associated with Succinylcholine in genetically deficient patients of plasma cholinesterase?
What is the primary adverse effect associated with Succinylcholine in genetically deficient patients of plasma cholinesterase?
What is the mechanism of action of Orphenadrine in causing analgesia and skeletal muscle relaxation?
What is the mechanism of action of Orphenadrine in causing analgesia and skeletal muscle relaxation?
What effect does Diazepam (Valium) have on muscle spasms?
What effect does Diazepam (Valium) have on muscle spasms?
Which drug causes hyperpolarization of the neuronal membrane by binding to GABAB receptors?
Which drug causes hyperpolarization of the neuronal membrane by binding to GABAB receptors?
What is the primary therapeutic use of Baclofen?
What is the primary therapeutic use of Baclofen?
What is a common adverse effect associated with Succinylcholine?
What is a common adverse effect associated with Succinylcholine?
How does Dantrolene exert its effect on skeletal muscles?
How does Dantrolene exert its effect on skeletal muscles?
What can occur when using Succinylcholine in conjunction with halothane in susceptible individuals?
What can occur when using Succinylcholine in conjunction with halothane in susceptible individuals?
Dantrolene causes an influx of calcium into the neuron, leading to hyperpolarization of the neuronal membrane.
Dantrolene causes an influx of calcium into the neuron, leading to hyperpolarization of the neuronal membrane.
Succinylcholine can be administered via intravenous continuous infusion.
Succinylcholine can be administered via intravenous continuous infusion.
Baclofen binds to GABA receptors to cause muscle spasms.
Baclofen binds to GABA receptors to cause muscle spasms.
Orphenadrine is a derivative of diphenhydramine and primarily acts as a stimulant.
Orphenadrine is a derivative of diphenhydramine and primarily acts as a stimulant.
Halothane combined with Succinylcholine may lead to hypothermia in genetically susceptible individuals.
Halothane combined with Succinylcholine may lead to hypothermia in genetically susceptible individuals.
Benzodiazepines enhance the action of glutamate, an excitatory neurotransmitter.
Benzodiazepines enhance the action of glutamate, an excitatory neurotransmitter.
In genetically deficient patients of plasma cholinesterase, Succinylcholine may cause prolonged paralysis due to slow hydrolysis.
In genetically deficient patients of plasma cholinesterase, Succinylcholine may cause prolonged paralysis due to slow hydrolysis.
Diazepam (Valium) is primarily used for treating hypertension.
Diazepam (Valium) is primarily used for treating hypertension.
Baclofen inhibits potassium influx into neurons, leading to muscle contraction.
Baclofen inhibits potassium influx into neurons, leading to muscle contraction.
Succinylcholine is a non-depolarizing neuromuscular blocking agent.
Succinylcholine is a non-depolarizing neuromuscular blocking agent.
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Study Notes
Cholinergic Antagonists
- Derived from Belladona alkaloid
- Central and peripheral activity
- Actions:
- Ophthalmic: mydriasis and cycloplegia
- GI system: antispasmodic
- Urinary system: enuresis
- CV: tachycardia
- Endocrine (secretory): xerostomia, xerophthalmia (dry mouth and eye)
- Therapeutic use:
- Ophthalmic: cycloplegic refraction, uveitis
- Antispasmodic
- Antidote: organophosphate intoxication (insecticides)
- Pharmacokinetics:
- Readily absorbed
- Partially metabolized in liver
- Eliminated in urine
- t 1/2 life of 4 hrs
- Adverse effects:
- Dry mouth
- Blurred vision
- Tachycardia
- Constipation
- Confusion
- Hallucinations
- Delirium
Scopolamine
- Belladona alkaloid with similar action to atropine
- Longer action in CNS
- Effective anti motion sickness/sedation
- Cycloplegic refraction, uveitis
Ipratropium / Tiotropium
- Quaternary derivative of atropine
- Used by inhalation for asthma and COPD
- Decreases smooth muscle contraction of bronchi
Tropicamide / Cyclopentolate
- Ophthalmic solutions
- Producing similar effects to atropine
Benztropine
- Centrally acting antimuscarinic agent
- Employed as adjuvant Tx in Parkinson Disease
- Minimizes dystonia in Tx with anti-psychotic medications
Darifenacin / Fesoterodine / Oxybutyin / Solifenacin / Tolterodine
- Synthetic atropine-like meds
- Used for overreactive bladder
- Increase capacity by lowering intravesical pressure
- Side effects:
- Dry mouth
- Constipation
- Blurred Vision (Diminished with regular use)
Nicotine
- Depolarize Ganglia ANS and striated muscle
- Low dose increases BP, HR, peristalsis, and secretions
- High dose decreases BP and diminishes muscular activity
- Neurochemical effects:
- Non-depolarizing (competitive) blockers
- Depolarizing blockers
Non-Depolarizing (Competitive) Blockers
- Curare (d-Tobocurarine,1st drug)
- Skeletal neuromuscular junction blocker
- Actions:
- Muscle paralysis
- Small muscles of face, eyes, fingers, limbs, neck, and trunk muscles
- The last one affected is the diaphragm
- Therapeutic use: adjuvant in anesthesia
- Pharmacokinetics: used IV, does not cross readily blood brain barrier
- Benefits: decrease concentration of general anesthetic drugs by achieving adequate muscle relaxation
Vecuronium / Rocuronium - Others
- Drug interactions:
- Cholinesterase inhibitors (neostigmine, etc.) overcome depolarizing action at low dose
- Aminoglycosides (gentamycin or tobramycin) inhibit acetylcholine release from neuromuscular junction – potentiate the effect of blockers
- Calcium channel blockers increase neuromuscular block of tebocurarine and other competitive blockers
Depolarizing Blockers
- Succinylcholine
- Attaches to nicotinic receptor acting like acetylcholine
- Depolarizing the neuromuscular junction persisting in cleft at [higher] for longer time followed by an altered repolarization
- 2 phases: twitch/flaccid paralysis during depolarization, desensitization during repolarization flaccid paralysis
- Actions: paralyzing process similar to non-depolarizing agents ending in respiratory muscles
- Therapeutic use: rapid endotracheal intubation during induction of anesthesia to avoid gastric aspiration
- Pharmacokinetics: rapid onset of short duration (minutes) due to hydrolysis by plasma cholinesterase
- Administered by IV continuous infusion
- Adverse effects:
- Hyperthermia
- Apnea in genetically deficient patients of plasma cholinesterase
Miscellaneous Muscle Relaxants
- Neural acting
- Benzodiazepines enhance or facilitate the action of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter
- Diazepam (Valium)*: use for muscle spasms
- Baclofen binds to GABAB receptors, causing influx of potassium into the neuron, leading to hyperpolarization of the neuronal membrane and decreased calcium influx at presynaptic nerve terminals
- Others:
- Dantrolene directly inhibits Ca++ release from sarcoplasmic reticulum
- Orphenadrine (methyl derivative of diphenhydramine) causes analgesia and skeletal muscle relaxation
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