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Medical Pharmacology Fall 2014 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

G-Protein α-Subunit Gs β-adrenoceptors; Histamine H2 receptors; Serotonin 5-HT4 receptors; Glucagon

A

↑adenylyl cyclase activity leading to ↑ levels of cyclic AMP

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2
Q

Gi1, Gi2,Gi3 α2-adrenoceptors; Muscarinic cholinergic M2 and M4; Serotonin 5-HT1; Opioids, cannbinoid

A

↓ adenylyl cyclase activity leading to ↓ levels of cyclic AMP; Open potassium channels

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3
Q

Gq Muscarinic cholinergic M1, M3 and M5; Serotonin 5-HT2; α1-adrenoceptors;

A

↑ phospholipase C activity leading to ↑ levels of IP3 and diacylglycerol that increase intracellular Ca2+

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4
Q

Target for GPCRs

A

Adenylyl cyclase, the enz responsible for Camp phospholipase C, the enzyme responsible for inositol phosphate and diacylglycerol (DAG) formation ion channels, particularly calcium and potassium channels

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5
Q

Therapeutic Uses of Direct-Acting Cholinergic Receptor Agonists Bethanechol

A

Postoperative ileus

Congenital megacolon

Urinary retention

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6
Q

Therapeutic Uses of Direct-Acting Cholinergic Receptor Agonists

Pilocarpine, Carbachol

A

Glaucoma

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7
Q

Edrophonium (Tensilon®)

, Tacrine (Cognex®),

Donepezil (Aricept®)

Galantamine (Reminyl®)

A

Indirect Acting Cholinomimetic Drugs:

Inhibitors of Acetylcholinesterase

Competitive Inhibitors

Reversible

Compete for ACh binding at the anionic site

Contains no ester linkage so that it is not hydrolyzed

Inhibition is rapidly reversible (increase Ach conc. will reverse their effect) DOA is not very long Tacrine discontinued due liver damage

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8
Q

Physostigmine,Rivastigmine (cross BBB)

Pyridostigmine, Neostigmine, (NOT CORSS BBB)

and Carbaryl, Propoxur and Aldicarb

A

Carbamate Inhibitors (garden products)

Reversible

They interact with 2 sites of the enzyme, the anionic site and they actually add carbamyl group to it.

Carbamyl ester linkage hydrolyzed to carbamylate enzyme Carbamyl moiety is slowly released - leads to long-lasting but reversible inhibition

Physostigmine and Rivastigmine are CNS permeable and used in treating Alzheimer’s disease

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9
Q

DFP (Isoflurophate); Echothiophate, (The only one therapeutically useful) Parathion, Tabun (GA), Sarin (GB), Soman (GF), VX (10x more potent than G-series)

A

Irreversible Inhibitors Used as insecticides and nerve gases Good CNS penetration (highly lipid soluble) Covalently phosphorylate the esteratic site of the enzyme (They phosphrylate that ser and the phosphrylation takes long time, good fortune) Phosphorylation is generally irreversible and enzyme must either be resynthesized or chemically reactivated by pralidoxime (2-PAM

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10
Q

Parathion,

A

Indirect Acting Cholinomimetic Drugs: Inhibitors of Acetylcholinesterase Irreversible Inhibitors Used as insecticides and nerve gases Good CNS penetration (highly lipid soluble) Covalently phosphorylate the esteratic site of the enzyme (They phosphrylate that ser and the phosphrylation takes long time, good fortune) Phosphorylation is generally irreversible and enzyme must either be resynthesized or chemically reactivated by pralidoxime (2-PAM

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11
Q

Tabun (GA)

A

Indirect Acting Cholinomimetic Drugs: Inhibitors of Acetylcholinesterase Irreversible Inhibitors Used as insecticides and nerve gases Good CNS penetration (highly lipid soluble) Covalently phosphorylate the esteratic site of the enzyme (They phosphrylate that ser and the phosphrylation takes long time, good fortune) Phosphorylation is generally irreversible and enzyme must either be resynthesized or chemically reactivated by pralidoxime (2-PAM

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12
Q

Sarin (GB),

A

Indirect Acting Cholinomimetic Drugs: Inhibitors of Acetylcholinesterase Irreversible Inhibitors Used as insecticides and nerve gases Good CNS penetration (highly lipid soluble) Covalently phosphorylate the esteratic site of the enzyme (They phosphrylate that ser and the phosphrylation takes long time, good fortune) Phosphorylation is generally irreversible and enzyme must either be resynthesized or chemically reactivated by pralidoxime (2-PAM

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13
Q

Soman (GF)

A

Indirect Acting Cholinomimetic Drugs: Inhibitors of Acetylcholinesterase Irreversible Inhibitors Used as insecticides and nerve gases Good CNS penetration (highly lipid soluble) Covalently phosphorylate the esteratic site of the enzyme (They phosphrylate that ser and the phosphrylation takes long time, good fortune) Phosphorylation is generally irreversible and enzyme must either be resynthesized or chemically reactivated by pralidoxime (2-PAM

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14
Q

VX (10x more potent than G-series)

A

Indirect Acting Cholinomimetic Drugs: Inhibitors of Acetylcholinesterase Irreversible Inhibitors Used as insecticides and nerve gases Good CNS penetration (highly lipid soluble) Covalently phosphorylate the esteratic site of the enzyme (They phosphrylate that ser and the phosphrylation takes long time, good fortune) Phosphorylation is generally irreversible and enzyme must either be resynthesized or chemically reactivated by pralidoxime (2-PAM

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15
Q

Carbaryl

A

Carbamate Inhibitors (garden products) Reversible They interact with 2 sites of the enzyme, the anionic site and they actually add carbamyl group to it. Carbamyl ester linkage hydrolyzed to carbamylate enzyme Carbamyl moiety is slowly released - leads to long-lasting but reversible inhibition Physostigmine and Rivastigmine are CNS permeable and used in treating Alzheimer’s disease

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16
Q

Propoxur

A

Carbamate Inhibitors (garden products) Reversible They interact with 2 sites of the enzyme, the anionic site and they actually add carbamyl group to it. Carbamyl ester linkage hydrolyzed to carbamylate enzyme Carbamyl moiety is slowly released - leads to long-lasting but reversible inhibition Physostigmine and Rivastigmine are CNS permeable and used in treating Alzheimer’s disease

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17
Q

Aldicarb

A

Carbamate Inhibitors (garden products) Reversible They interact with 2 sites of the enzyme, the anionic site and they actually add carbamyl group to it. Carbamyl ester linkage hydrolyzed to carbamylate enzyme Carbamyl moiety is slowly released - leads to long-lasting but reversible inhibition Physostigmine and Rivastigmine are CNS permeable and used in treating Alzheimer’s disease

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18
Q

Organ System Effects of Cholinesterase Inhibition Cardiovascular

A

Bradycardia Decreased Cardiac Output (CO) Hypotension (modest except in toxic doses

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19
Q

Organ System Effects of Cholinesterase Inhibition Respiratory System

A

Bronchoconstriction Increased secretion (copious) Paralysis of diaphragm

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20
Q

Organ System Effects of Cholinesterase Inhibition GI Tract

A

Increased tone Increased motility Increased secretions

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21
Q

Organ System Effects of Cholinesterase Inhibition Skin

A

Increased sweating

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22
Q

Organ System Effects of Cholinesterase Inhibition Eye

A

Miosis Near accommodation

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23
Q

Organ System Effects of Cholinesterase Inhibition Central Nervous System

A

Tremor Anxiety Confusion Convulsions Coma

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24
Q

Therapeutic Uses of Cholinesterase Inhibitors

A

Glaucoma Postoperative ileus, congenital megacolon, urinary retention Diagnosis and Treatment of Myasthenia Gravis Surmounting effects of competitive neuromuscular blocking agents Treatment of Alzheimer’s disease (increasing adverse cardiovascular events!!!) Treatment of Atropine poisoning (and al types of anticholinergic poisoning)

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25
Diagnosis and Treatment of Myasthenia Gravis
Therapeutic Uses of Cholinesterase Inhibitors
26
Postoperative ileus, congenital megacolon, urinary retention
Therapeutic Uses of Cholinesterase Inhibitors
27
Glaucoma
Therapeutic Uses of Cholinesterase Inhibitors
28
Surmounting effects of competitive neuromuscular blocking agents
Therapeutic Uses of Cholinesterase Inhibitors
29
Treatment of Alzheimer’s disease (increasing adverse cardiovascular events!!!)
Therapeutic Uses of Cholinesterase Inhibitors
30
Treatment of Atropine poisoning (and al types of anticholinergic poisoning)
Therapeutic Uses of Cholinesterase Inhibitors
31
Treatment of Cholinesterase Inhibitor Poisoning
Contains: 1) Atropine to block M R effect 2) 2PAM becasue of the organophophate exposure, so 2PAM reactiviate the enzyme. Pralidoxime (2-PAM) for reactivation of enzyme (oxime group has high affinity for phosphorus) and is effective at the neuromuscular junction It does not take care for the N side so the paralysis of diaphragm and the CNS effects are problematic and need supportive therapy
32
Methacholine
Therapeutic use if Direct-Acting cholinergic receptor agonist Bronchial Reactivity
33
Hexamethonium
Nondepolarizing Ganglionic Blocking Agent Noncompetitive antagonist of the NN receptor (allosteric antagonism) Not used therapeutically but experimentally. Blocks the open state of the ion channel
34
Trimethaphan
Nondepolarizing Ganglionic Blocking Agent Competitive Antagonist of the Nn receptor Used therapeutically
35
Mecamylamine
Nondepolarizing Ganglionic Blocking Agent Competitive Antagonist of the Nn receptor Used therapeutically
36
Nicotine
Depolarizing Ganglionic Blocking Agents Agonist at NN receptors (low concentrations) Stimulates release of catecholamines from the adrenal medulla Stimulates baroreceptors leading to vasoconstriction and tachycardia Higher concentrations lead to ganglionic blockade that proceeds through two distinct phases
37
Characteristics of Neuromuscular Blocking Drugs
Agents do not produce analgesia or anesthesia Most are poorly absorbed (quaternary ammonium compounds) and do not cross BBB Usually administered intravenously
38
d-Tubocurare; pancuronium, vecuronium, rapacuronium, rocuronium; and cisatracurium, atracurium, and mivacurium
Non-depolarizing Neuromuscular Blocking Drugs Competitive inhibition of ACh binding at the nAChR (NM) receptor (Stabilizing blockade) Rapidly developing muscle weakness followed by flaccid paralysis Curare is least selective among the agents as it also produces some ganglionic blockade and induces histamine release but no longer available in US (historical significance See notes
39
**Succinylcholine** **Nicotine?**
Depolarizing Neuromuscular Blocking Drugs Inhibition of activation of the NM receptor similar to the blockade of NN receptor (Desensitization) Muscle fasciculations (initial depolarization followed by increasing weakness leading to flaccid paralysis) Desensitization occurs when end-plate is repolarized but not able to be activated by agonists Blockade of initial part of phase II desensitization will not be reversed by cholinesterase inhibitors
40
**Therapeutic Uses of Neuromuscular Blocking Agents**
Relax skeletal muscle during surgery Permit reduction in anesthetic dose Assist with orthopedic procedures Facilitate procedures involving skeletal muscle (e.g. intubation, laryngoscopy, endoscopy, ECT)
41
**Comparison of Characteristics of Long Acting Isoquinolines with other NM Blocking Agents**
42
43
**Drug cuases Prolonged apnea **
•Adverse Effects Associated with Neuromuscular Blocking Agents Succinylcholine
44
**Adverse Effects Associated with Neuromuscular Blocking Agents**
* Prolonged apnea (Succinylcholine) * Increased intraocular pressure, increased intragastric pressure, hyperkalemia (can produce cardiac arrest) * Muscle pain * Malignant Hyperthermia (combination of inhalational anesthetic/depolarizing agent)
45
Effects of Cholinergic Receptor Stimulation: Muscarinic Receptors ## Footnote **Wet and Wild (Mostly GI)**
* Nausea, belching, vomiting, cramps and defecation * Urination * Salivation, increased sweating * Bronchoconstriction, increased mucociliary secretion * Increased lacrimation, rhinorrhea
46
Effects of Cholinergic Receptor Stimulation: Muscarinic Receptors **Cardiovascular System (M2, M3)**
•Decreased heart rate and rate of conduction
47
Effects of Cholinergic Receptor Stimulation: Muscarinic Receptors **Eye (M3)**
* Contraction of iris sphincter (miosis) * Contraction of ciliary muscle (accommodation)
48
Organ System Effects of Muscarinic Cholinergic Receptor Antagonism **Central Nervous System (mainly scopolamine)**
•Low Dose –Drowsiness –Amnesia •Dreamless sleep •High Dose (Jimson weed, Devil’s breath, burundanga, Borrachero tree): –Excitement –Confusion/disorientation –Hallucinations –Coma –Loss of intention
49
Organ System Effects of Muscarinic Cholinergic Receptor Antagonism **Eye**
–Pupillary dilation (mydriasis) –Paralysis of accommodation (cycloplegia) –Increased intraocular pressure
50
Organ System Effects of Muscarinic Cholinergic Receptor Antagonism **•Cardiovascular System**
–Tachycardia –Antagonizes vasodilation and hypotension produced by choline esters
51
Comparison of Muscarinic Receptor Blockade versus Occupancy
The effect with increase dose of Atropine. The effect does mimick the R occupancy except for early stages. The best guess is its interacting with presynaptic M2 R
52
Organ System Effects of Muscarinic Cholinergic Receptor Antagonism **•Respiratory System**
–Bronchodilation –Inhibits secretion and reduces mucociliary clearance –Complete blockade of salivary secretion
53
•Organ System Effects of Muscarinic Cholinergic Receptor Antagonism **•GI and Urinary Tract**
–Inhibition of GI tone and peristalsis –Inhibition of gastric acid secretion –Urinary retention
54
* Organ System Effects of Muscarinic Cholinergic Receptor Antagonism * **Skin**
–Inhibits sweating
55
Relative Sensitivity to Muscarinic Cholinergic Receptor Blockade
Atropine, the protypuical antimuscranic agent. Increase in Atropine's dose measures 4 outcomes: decrease in salivation decrease in micturition decrease in accomodation increase in H.R
56
To which activity does Atropine has the greater potency?
Dry mouth is the hallmark side effect for Atropine. (decrease in salivation)
57
**Ipratropium (Atrovent®)**
Synthetic Muscarinic Antagonists Interesting drug. It is a solution that you inhaled
58
**Tiotropium (Spiriva®)**
Synthetic Muscarinic Antagonists 4° amines It is inhaled powder. Why? Because these agents are 4° amines that are not soluble in water. So they use a solvent contains soya lecithin. contraindicated in patients hypersensitive to soya lecithin or other food products (soy bean or peanuts) and used with caution in patients with prostatic hypertrophy
59
**•Tolteridine •Oxybutynin •Trospium Darifenacin**
Prototypical Synthetic Muscarinic Antagonists Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
60
Tolteridine (Detrol®) and Fesoterodine (Toviaz®), Oxybutynin (Ditropan®, Oxytrol®, Gelnique®), Trospium (Spasmex®), Flavoxate (Urispas®), Darifenacin (Enablex®) and Solifenacin (VESIcare®)
•Synthetic Muscarinic Antagonists Used to treat overactive bladder
61
•**Solifenacin**
Synthetic Muscarinic Antagonists Used to treat overactive bladder being most selective for M3 R Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
62
Solifenacin, Darifenacin and Oxybutynin are somewhat selective for M3 receptors with Darifenacin being most selective
Synthetic Muscarinic Antagonists are somewhat selective for M3 receptors with Darifenacin being most selective (selective but not specific) Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
63
•**Tolteridine**
•Synthetic Muscarinic Antagonists Used to treat overactive bladder Appear lest selective for M3 R Caution for most of the agents when used concomitantly with CYP3A4 inhibitors extended durations of action (daily dosing)
64
**•Fesoterodine**
Synthetic Muscarinic Antagonists Used to treat overactive bladder appear less selective M3 extended durations of action (daily dosing) Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
65
**•Oxybutynin**
•Synthetic Muscarinic Antagonists •Used to treat overactive bladder somewhat selective for M3 receptors Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
66
**•Trospium**
•Synthetic Muscarinic Antagonists Used to treat overactive bladder Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
67
**•Darifenacin**
•Synthetic Muscarinic Antagonists •Used to treat overactive bladder •Darifenacin being most selective for M3 receptors Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
68
•Flavoxate
•Synthetic Muscarinic Antagonists Used to treat overactive bladder Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
69
•**Solifenacin**
* Synthetic Muscarinic Antagonists * somewhat selective for M3 receptors Caution for most of the agents when used concomitantly with CYP3A4 inhibitors
70
**Homatropine**
Synthetic Muscarinic Antagonists –Short acting analogue of atropine –Used to produce brief mydriasis and cycloplegia –Combined with hydrocodone as Hycodan® for use as an antitussive Duration 1-3 days
71
**•Cyclopentolate (Cyclogyl®)**
•Synthetic Muscarinic Antagonists –Ultra short acting agents for ophthalmological examination –Short-lived mydriasis and cycloplegia Duration 1 day
72
**Tropicamide (Mydriacyl Ophthalmic®)**
•Synthetic Muscarinic Antagonists –Ultra short acting agents for ophthalmological examination –Short-lived mydriasis and cycloplegia Duration 0.25 days
73
•Therapeutic Uses of Muscarinic Cholinergic Receptor Antagonists ## Footnote
**Prevent motion sickness** (Scopolamine) – transdermal patches **Produce sedation, amnesia and tranquilization** (hallucinogenic properties exploited as well) Produce mydriasis and cycloplegia **Inhibit salivation and respiratory tract secretions** (e.g. hyperhidrosis or prior to and during surgery) **Treatment of asthma and COPD** Treatment of cholinomimetic poisoning (especially bradycardia and hypotension)
74
Why anitmascarnic agents are C/I with patients with narrow angle glaucoma?
Because these agents dilate the pupil, so they move the iris away from the angle of the eye. So in patient who has narrow angle glaucoma, that angle is already compressed. Now if dilate the iris with these agents, you will block the out flow facility of the eye preventing fluid from passing.
75
How to overcome the anitmascarnic blocking effects?
With Anitacytlcholinesterase inhibitor to increase the level of Ach in the synaptic cleft

Medical Pharmacology Fall 2014 (6 decks)

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