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.Pharmacology > TO RECALL 2 > Flashcards

TO RECALL 2 Flashcards

1
Q

General NSAID MOA

A

Inhibiting the prostaglandin (PG) G/H synthase enzyme or cyclooxygenase (COXs)

act as antipyretic, analgesic, and anti-inflammatory

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2
Q

Drug:

Aspirin

A
  • only irreversible inhibitor of the COX enzymes (COX-1 and COX-2)
  • has cardioprotective effects
  • cannot be given to children and young adults below 20 y.o. due to Reye syndrome
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3
Q

Drug:

Acetaminophen (paracetamol)

A
  • effective antipyretic and analgesic
  • partly inhibits COXs - reversible
  • NSAID with weak anti-inflammatory activity
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4
Q

Side effects of inhibition of COX-1

A

(1) Gastric adverse events - COX-1 is the dominant cytoprotective isoform in gastric epithelial cells

(2) Bleeding - COX-1 forms TxA2 in platelets which amplifies platelet activation and constricts blood vessels at site of injury

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5
Q

Side effects of COX-2 inhibition

A

(1) exacerbate hypertension - COX-2 plays important roles in blood pressure regulation

(2) increases likelihood of thrombotic events - COX-2 act as endogenous inhibitors of hemostasis

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6
Q

Aside from the usual Neurotransmitters, enumerate additional peptides, purines, and small molecules that can be used.

A

(Peptides): enkephalin, substance P, neuropeptide Y, vasoactive intestinal polypeptide, somatostatin

(Purines): ATP and Adenosine

(Small molecules): Nitric Oxide

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7
Q

In a neuron, the resting potential is (1), the threshold potential is (2), the intracellular ion is (3), and the extracellular ion is (4),

A

(1) -70 mV
(2) - 55 mV
(3) K+ , potassium has a high concentration inside the cell
(4) Na+, sodium has a low concentration inside the cell but have a high concentration outside

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8
Q

Posion

Tetrodotoxin

A
  • secretions from puffer fish
  • block the voltage gated Na+ channel which prevents depolarization
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9
Q

Poison

Saxitoxin

A
  • secretions from shellfish
  • block the voltage gated Na+ channel which prevents depolarization
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10
Q

Poison

Batrachotoxin

A
  • toxin from the South American Frog
  • extremely potent steroidal alkaloid
  • it increases the permeability of Na+ channel causing hyper-depolarization paralysis
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11
Q

Poisons

Scorpion Toxin

A

Causes persistent depolarization by inhibiting its deactivation

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12
Q

Drug

Hemicholinium

A
  • blocks CHT1 (choline transporter 1 or SLC5A7) a Na+ and Cl- dependent transporter in presynaptic membranes of cholinergic neurons
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13
Q

Drug

Vesamicol

A
  • functions as a noncompetitive and reversible inhibitor of acetylcholine uptake in storage vesicles
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14
Q

Drug

Botulinum toxin

A
  • blocks ACh release by interfering with the machinery of transmitter release (exocytosis of storage vesicle to release neurotransmitters)
  • cleaves SNARE proteins
  • at Neuromuscular Junction (NMJ)
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15
Q

Poison

Tetanus toxin

A
  • similar to botulinum toxin but acts in the CNS
  • cleave SNARE protein synaptobrevin to block exocytosis and release of acetylcholine
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16
Q

Drug

ACE inhibitors

A
  • block acetylcholinesterase to increase interaction of post synaptic neuron with acetylcholine
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17
Q

Drug

Trimethaphan and Mecamylamine

A

Neuronal nicotinic antagonists

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18
Q

Muscarinic Receptors (M1, M2, M3, M4, M5)

A
  • G protein coupled
  • M1, M3, M5 - increase cAMP
  • M4, M5 - decrease cAMP
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19
Q

Predominant parasympathetic receptor subtype in the heart

A

Muscarinic receptor (M2)

20
Q

Muscarinic receptors (M1, M3, and M5) take effect by what signaling pathway?

A

(1) Gq/11
(2) stimulates the PLC-IP3/DAG-Ca2+ pathway
(3) activation of PKC and Ca2+ sensitive enzymes or PLA2 leading to the release of arachidonic acid and consequent eicosanoid synthesis

21
Q

Muscarinic receptors (M2 and M4) take effect by what signaling pathway

A

(1) Gi and G0
(2) resulting to inhibition of adenylyl cyclase
(3) decrease in cellular cAMP, activation of inwardly rectifying K+ channels, and inhibition of voltage-gated Ca+ channels
(4) hyperpolarization and inhibition of excitable membranes

22
Q

Tyrosine acted on by tyrosine hydroxylase (3-hydroxylated) and decarboxylated produces

A

Dopamine

23
Q

Dopamine is converted to Norepinephrine via

A

Dopamine Beta-hydroxylase

24
Q

Norepinephrine acted on by N-methyltransferase produces

A

Epinephrine

25
Q

Drug

Reserpine

A

Inhibits monoamine transport into storage vesicles leading to depletion of catecholamine from sympathetic nerve endings in the brain

26
Q

Drug

Fluoxetine

A
  • inhibit SERT
  • selective 5HT reuptake inhibitors
27
Q

Drug

Normetanephrine

A
  • inhibitors of OCT3 (organic cation transport for uptake of epinephrine, SLC 22A3)
28
Q

Drug

Alpha-methyltyrosine

A
  • inhibition of tyrosine hydroxylase
  • depletes norepinephrine used in sympathetic signaling
29
Q

Drug

Methyldopa

A
  • converted to alpha-methyl-NE to displace norepinephrine in its function as an alpha 2 agonist
  • treatment for hypertension
30
Q

Drug

Cholinomimetic for Muscarinic receptors

A

Methacholine and bethanachol

31
Q

Drug

Cholinomimetic for Nicotinic receptors

A

Nicotine, epibatidine, cytisine

32
Q

Drug

Phenylephrine

A

Selective alpha 1 agonist

33
Q

Drug

Clonidine

A

Sympathomimetic - alpha 2 receptors

34
Q

Drug

Oxymetazoline

A

Nonspecific alpha receptor agonist (alpha 1 & 2)

35
Q

Drug

Dobutamine

A
  • Beta 1 agonist
  • selective cardiac stimulation
36
Q

Drug

Terbutaline, albuterol, metaproterenol

A

Beta 2 receptor agonist

37
Q

Drug

Nonselective Beta agonist

A

Isoproterenol

38
Q

Drug

Atropine

A

Blocks muscarinic receptors

39
Q

Drug

d-Tubucurarine and atracurium

A
  • Neuromuscular blockade
  • blocks muscular nicotinic receptors
40
Q

Drug

Trimethaphan

A
  • Ganglionic blockade
  • blocks neuronal nicotinic receptors
41
Q

Drug

Phenoxybenzamine

A
  • nonselective irreversible alpha receptor blockade
42
Q

Drug

Phentolamine

A

Nonselective reversible alpha receptor blockade

43
Q

Drug

Prazosin, Terazosin, doxasozin

A
  • selective reversible alpha 1 receptor blockade
44
Q

Drug

Yohimbine

A
  • selective alpha 2 receptor blockade
45
Q

Drug

Propranolol

A
  • nonselective beta receptor blockade
46
Q

Drug

Metoprolol and atenolol

A
  • selective beta 1 receptor blockade
47
Q

Drug

NSAIDs that are classified as salicylates

A
  1. Aspirin
  2. Diflunisal

.Pharmacology (55 decks)

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