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Medications > Anti-histamine and NSAIDs > Flashcards

Anti-histamine and NSAIDs Flashcards

0
Q

H2 receptor mechanism

A

Gs coupled: increase cAMP

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1
Q

H1 receptor signaling mechanism

A

Gq couples: PLC > IP-3, DAG (mobilizes Ca2+ > histamine degranulation, smooth muscle constriction)

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2
Q

H3 receptor mechanism

A

Gs coupled: increase cAMP

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3
Q

H4 receptor mechanism

A

Gs coupled: increase cAMP

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4
Q

Vascular smooth muscle (H1, (H2))

A

histamine induced NO release > SM relaxatoin + vasodilation

Symptom: hypotension, flushing, headache, anaphylaxis

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5
Q

Endothelium (H1)

A

Induce actin/myosin contraction, separate endothelial cells

Symp:edema

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6
Q

Cardiac muscle (H1)

A

Decreased HR and atrial contractility

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7
Q

Cardiac muscle (H2)

A

Increased HR and contractility

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8
Q

Bronchiolar smooth muscle (H1)

A

Constriction

Symp: decreased airway size + difficulty breathing

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9
Q

Uterine smooth muscle (H1)

A

Constriction

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10
Q

Gastric smooth muscle (H1)

A

constriction

Symp: diarrhea

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11
Q

Sensory nerves (H1)

A

stimulation

Symp: pain + itching

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12
Q

CNS in hypothalamus (H1)

A

Arousal

Symp: increased wakefulness

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13
Q

CNS in emetic center (H1)

A

emesis

Symp: vomiting, nausea

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14
Q

CNS (H1 + H2)

A

Effects on thirst, BP, perception of pain

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15
Q

Gastric secretion (H2)

A

Increased acid production, pepsin and IF

Symp: mucosal erosion + ulceration

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16
Q

Cromolyn (Intal)

A

Prophylactic in longer term maintenance therapy fo rasthma
Inhibits degranulation of mast cells (inhibit Ca2+ channels, inhibit Cl- channels > decreased nerve activity + cough)
Lacks utility due to topical absorption of poorly soluble salts (inhaled powder aerosol)

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17
Q

Nedocromil (Tilade)

A

Prophylactic in longer term maintenance therapy fo rasthma
Inhibits degranulation of mast cells (inhibit Ca2+ channels, inhibit Cl- channels > decreased nerve activity + cough)
Lacks utility due to topical absorption of poorly soluble salts (inhaled powder aerosol)

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18
Q

H1 Receptor antagonists

A

Act as inverse agonist (block histamine at H1 receptors)
Uses: allergic rhinitis and uticaria (H1 antagonist), motion sickness/emesis (H1 antagonist + antimuscarinic effect)
SE: sedation (1st Gen Drugs: CNS Hypothalamic response, cross BBB)
Non-H1 effects: first gen H1 anta similar to muscarinic cholinoreceptor (dry mouth, urinary retention, tachycardia), a-adrenoceptor (orthostatic hypotension), anit-serotonin (increased appetite), local anesthetic (block Na channels)

19
Q

Diphenhydramine (Benadryl)

A

1st Gen: H1 antagonist = antihistamine
Other Uses: motion sickness
Also a muscarinic antagonists (prevent parasympathetics)

20
Q

Dimenhydrinate (Dramamine)

A

1st Gen: H1 antagonist = antihistamine
Other Uses: motion sickness
Salt of diphenhydramine

21
Q

Cyclizine (Marezine)

A

1st Gen: H1 antagonist = antihistamine

Other Uses: motion sickness

22
Q

Promethazine (Phenergan)

A

1st Gen: H1 antagonist = antihistamine

Other Uses: antiemetic

23
Q

Most effective drugs for motion sickness and emesis

A

promethazine, cyclizine and diphenhydramine

24
Q

Loratadine

A

(Claratin): 2nd Gen antihistamine

Highly selective for H1 sites, few anti-cholinergic SE, poorly cross BBB > less sedative effects

25
Q

Cetrizine

A

(Zyrtec): 2nd Gen antihistamine

Highly selective for H1 sites, few anti-cholinergic SE, poorly cross BBB > less sedative effects

26
Q

Fexofenadine

A

(Allegra): 2nd Gen antihistamine

Highly selective for H1 sites, few anti-cholinergic SE, poorly cross BBB > less sedative effects

27
Q

Prostaglandin E2

A

Site of synthesis: Most tissues
Half-life: 30 sec
Oppose thromboxanes > suppress TXA

28
Q

Prostaglandin I2 (prostacyclin)

A

Site of synthesis: Endothelium, vascular smooth muscle
Half-life: 3 min
Oppose thromboxanes > suppress TXA

29
Q

Thromboxane A2

A

Site of synthesis: Platelets, macrophages
Half-life: 30 sec
Proinflammatory

30
Q

Aspirin

A

Acetyl salicylic acid (Irreversible inhibitor of COX-1 + COX-2) > 15 min > salicylic acid (reversible inhibitor of both)
More potent inhibitor or COX-1
COX-2 is responsible for prostanoid production during inflammation
Use: OTC analgesic/antipyretic, CARDIOVASCULAR PROPHYLAXIS

31
Q

Ketorolac (Toradol)

A

Selectivity of COX-1 vs COX-2 = 395

Use: post surgical analgesic

32
Q

Indomethacin (Indocin)

A

Parenteral (high potency for COX-1)
Selectivity of COX-1 vs COX-2 = 10
Use: Rx arthritis/anti-inflammatory
high frequency of intolerance

33
Q

Naproxen (Aleve, Bayer)

A

Selectivity of COX-1 vs COX-2 = 3.8

Use: aspirin: analgesic/antipyretic, Rx anti-inflammatory

34
Q

Ibuprofen (Motrin, Advil)

A

Selectivity of COX-1 vs COX-2 = 2.6

Analgesic/antipyretic

35
Q

Diclofenac (Voltaren, Cataflam)

A

Selectivity of COX-1 vs COX-2 = 0.3 (More potent towards COX-2)
combined with misoprostol (Arthrotec)
Uses: Rx arthritis/anti-inflammatory

36
Q

Etodolac (Lodine)

A

Selectivity of COX-1 vs COX-2 = 0.1

Use: Rx arthritis

37
Q

Meloxicam (Mobic)

A

Selectivity of COX-1 vs COX-2 = 0.04

Use: Rx arthritis

38
Q

Misoprostol

A

PGE1 analog: used to protect against COX-1 inhibition by NSAIDs to allow prostglandins for the decreases in acid production, increased mucus formation in the stomach = prevent ulcers

39
Q

Acetaminophen (tylenol)

A

Non-selective Cox inhibitor
Activity reduced in presence of peroxide (often located at inflamed site)
Uses: analgesic and antipyretic (no anti-inflammatory activity)
SE: hepatotoxicity with overdose

40
Q

Celecoxib (Celebrex)

A

Only legal US Cox-2 selective NSAID: 10X selectivity
Uses:analgesic, rheumatoid arthritis
Reduces incidene of GI effects
SE: for all COX-2 selective inhibitors = increased cardiovascular events: hypertension, heart attack, stroke

41
Q

Rofecoxib (Vioxx)

A

Cox-2 Selective NSAID: 200X selectivity (most selective)

Uses: analgesis, Rx arthritis

42
Q

Valdecoxib (Bextra)

A

similiar to rofecoxib: COX-2 selective inhibitor: 200X selectivity

43
Q

Zileuton

A

Leukotriene pathway synthesis inhibitor: inhibits 5-lipoxygenase > no LTB4/LTD4 synthesis
Uses: long-term maintenance therapy for asthma (oral)
SE: liver toxicity, inhibited activity of Cyt P450 1A2, 2C9, 3A4

44
Q

Zafirlukast (Accolate) + Montelukast (Singular)

A

Longer term asthma maintenance

LTD4 receptor antagonist > reduced bronchoconstriction + edema from inflammatory response

Medications (3 decks)

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