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Pharmacology > GI Meds > Flashcards

GI Meds Flashcards

1
Q

Histamine
Where/how its synthesized
Storage released in resp to

A

Synth in tissues, decarboxylation of histamine. Stored in vesicles in mast cells (skin, lung, gastric mucosa) and circ basophils. Released in rep to antigen-Ab rxn/drugs

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2
Q

Histamine
3 effects in body
Mediated by

A

Inflammatory mediator, reg gastric acid secretion, reg neurotransmission. Doesnt readily cross BBB (no cns fx). Receptors H1, 2, 3

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3
Q

H1 and H2 antagonists dont inhibit what, do what

A

Dont inhib release of histamine, block response to histamine

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4
Q

H1 does what overall

A

Smooth muscle contraction lung, gi, vascular, release of NO, sensory nerve stim

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5
Q

H1 fx

Lungs

A

Bronchoconstriction, asthma/bronchitis, inc a/w resistance

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6
Q

H1 fx vascular smooth muscle

A

Dilation leads to hypotension and erythema

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7
Q

H1 fx vascular endothelium
Peripheral nerves
Heart

A

Inc cap permeability, edema
Sensitization, itching, pain, sneezing
In AV node, slow HR by slowing conduction

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8
Q

H2 receptor

Where they are

A

Gastric parietal cells, cv muscle, mast cells

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9
Q

H2 receptor

Action in heart and coronary vasculature

A

+ inotropic/chronotropic. Inc rate and contrac. Vasodilated heart vessels, offsets H1 constriction

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10
Q

H2 receptor
A/w fx
Activ cell level in stomach

A

Relaxes bronchial smooth muscle

Inc camp, activates proton pump of parietal cells to secrete h ions

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11
Q

H2 receptor

Fx in stomach

A

Gastric acid secretion, PUD and gerd

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12
Q

H3 receptor locations

Stim causes what

A

Heart and presynaptic postganglionic SNS fibers

Inhib of synthesis and release of histamine

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13
Q

H3

Activity impaired by what, avoid what

A

H2 antagonists, leads to inc histamine release. Avoid admin of these agents w a histamine releasing drug like atracurium

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14
Q

H1/2 antagonists

Histamine receptors that they occupy, about inhibition

A

Transmembrane G protein coupled. Competitive and reversible inhibition

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15
Q

H1 antag used for

H2 antag used for

A

1- allergic rhinitis

2- inhib gastric acic fluid secretion

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16
Q

H1 receptor antag

Diff b/w first and second gen

A

1st- sedation, activ muscarinic, serotonin and alpha receptors
2nd- non drowsy, decreases cns toxicity

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17
Q

H1 receptor antag
Uses
Not used for

A

Rhinitis, conjunctivitis, urticaria, pruritis.

Not effec for systemic anaphylaxis or asthma

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18
Q

H1 receptor antag

Used for __ /___ AND ____ specific ones

A

N/v, motion sickness. Diphenhydramine, dimenhydrinate, meclizine, promethazine

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19
Q

H1 receptor antag for insomnia

A

Diphenhydramine and doxylamine

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20
Q

H1 antihistamines
About 1st gen: 2
5 ex

A

Lipophilic, neutral and physio pH.

Diphenhydramine, hydroxyzine, chlorpheniramine, promethazine, doxepin

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21
Q

2nd gen h1 antihistamines
About drug 2
Ex 4

A

Albumin binding, ionized at physio pH.

Loratidine, desloratidine, acrivastine, fexofenadine

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22
Q

H1 antag
___ absorption
Cmax when
Protein binding

A

Excellent
2-3hrs
78-99%

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23
Q

H1 antag

Metab by what

A

Cyp 450

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24
Q

H1 antihistamines AE
Toxicities 2
___ effects

A

CNS (sedative), cardiac (QTi prolong)

Anticholinergic: pupil dilation, dry eyes/mouth, urine ret

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25
Q

H2 antagonists
MOA
4 agents

A

Competitive antagonist at h2 receptor, suppresses gastric acid sec by parietal cells. Cimetidine, nizatidine, ranitidine, famotidine

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26
Q 
H2 antagonists 
Decreases intracellular \_\_ 
Least potent 
Most potent 
No effect where
A

CAMP
Cimetidine
Famotidine
LES tone/gastric emptying

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27
Q

H2 antag work on which pump

A

H K atpase

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28
Q

H2 antagonists effects

A

Tx duodenal ulcers and gerd, chemoprophylaxis prior to induction of GA

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29
Q

Chemoprophylaxis doses/when to give

Cimetidine

A

300 mg po/iv 1-2hrs preop

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30
Q

Chemoprophylaxis doses/when to give

Famotidine

A

20-40 mg po/20 mg iv am of surgery

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31
Q

Chemoprophylaxis doses/when to give

Ranitidine

A

150 mg po or 50 mg iv

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32
Q

H2 antagonists

No effect where

A

No effect on gastric pH. Unpredictable volume effect

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33
Q

H2 antagonists
Metab
Cmax

A

Rapid oral abs, 1st pass metab, 50% bioavailability

1-3 hrs

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34
Q

H2 antagonists
Protein binding
BBB
Elim

A

15-35%
All 4 cross it
1.5-4 hrs

35
Q

H2 antagonists
Which one renal exc
Metabolism primarily

A

Nizatidine

Other 3 hepatic metab

36
Q

H2 antag SE
Which 2 things inc SE severity
May have transient elev of

A

Multisystem disease and inc age

LFTs

37
Q

H2 Antagonists
Avoid rapid admin of __ and __, why
Give over what time period

A

Cimetidine and ranitidine
Hypotension and bradycardia
15-30 min

38
Q

H2 antagonists

__ may be given over 2 min

A

Famotidine

39
Q

H2 antagonists

Decreases metab of what

A

Drugs w hepatic metab. Propranolol and diazepam

40
Q

H2 antagonists

Cimetidine may slow metab of __ and other __

A

Lidocaine, drugs

41
Q

Goals of PUD therapy 3

A

Reduce gastric acidity, enhance mucosa, elim h pylori

42
Q

Drug tx PUD
For acid
Mucosa
H pylori

A

H2 antag, PPI, and anticholinergics for acid sec inhib. Antacids to neutralize. Mucosa protection: sucralfate, bismuth, prostaglandins. Abx

43
Q

PPI

Block what

A

K h ATPase

44
Q

PPI
__ absorption
Conversion, where

A

Rapid

Prodrug to active drug in parietal cell canaliculus

45
Q 
PPI 
\_\_ bond w proton pump 
\_\_ half life 
Metab 
Crosses \_\_
A

Covalent
Short
Cyp 2c19 and 3a4
Crosses placenta

46
Q

PPI

AE

A

HA, GI disturb, nausea, enteric infections. Long term unknown, maybe carcinoid tumors

47
Q

PPI

Indic for what

A

PUD w h pylori
Hemorrhagic ulcers
PUD in pt who req nsaid use

48
Q

Dicyclomine
MOA
__ effective than h2 antag and PPI
AE

A

Musc ach antag, dec acid sec
Less
Dry mouth, constip, blurry vision, cardiac arrhythmia, urine ret

49
Q

Where anticholinergics work in parietal cell

A

Block acetylcholine and Gastrin

50
Q

Sucralfate
What it is
How it works

A

Salt of sucrose sulfate and al oh. Forms gel that binds to + charged proteins (albumin and fibrinogen), sticks to ulcer areas. Protects tissue from pepsin, acid, and bile salts

51
Q

Sucralfate
Doesnt do what
Does do what
AE

A

Doesnt alter gastric ph
Does relieve symptoms
Constip, little systemic absorp, big pills and frequent admin, drug interactions (binds to them)

52
Q

Colloidal bismuth
Used in what
Protects how

A

PUD. Coating agent. Protects mucosa from acid and pepsin degradation, forms barrier. Stim mucosal bicarb and prostaglandin, impedes h pylori

53
Q

Prostaglandins
Agent
Does what
AE/contra

A

Misoprostal, pg analogue. Prevents nsaid induced ulcers. Abd discomfort and diarrhea. Pregnancy

54
Q

Tx h pylori

Triple therapy

A

Amoxicillin, clarithromycin, PPI

55
Q

H pylori

Quadruple therapy

A

Tetracycline, metronidazole, PPI, bismuth

56
Q

Antacids

Inc pH to what

A

5

57
Q

AE of antacids, 4 agents

A

Constip, diarrhea, electrolyte abn

Al oh, mg oh, na hco3, ca co3

58
Q 
Na citrate/bicitra 
What kind of antacid 
Onset 
Dose 
PH
A

No particulate, clear
15-30 min to facial mixing and emptying
15-30 ml po
8.4

59
Q

Reglan
MOA
__ only, __ unchanged

A

Dopamine antagonist

Kinetic, pH

60
Q

Reglan

What it does to GI tract 3

A

Cholinergic stim. Inc LES tone, inc gastric/small bowel motility, relaxes pylorus and duodenum

61
Q

Reglan
Post synaptic release of __
Opposed by what

A

Ach. Atropine and glyco

62
Q

Reglan
___ effects
Stim __ secretion
__ __ effects

A

CNS effects, EPS
Prolactin
Anti emetic

63
Q 
Reglan 
Absorption 
Peak 
E 1/2 
Excretion
A

Rapid po
40-120 min
2-4 hrs
Renal exc, 40% unchanged

64
Q

Reglan uses

4

A

Dec gastric fluid vol
Antiemetic
Gastroparesis
Gerd symptomatic tx

65
Q

Reglan periop

When/how to give before induction

A

10-20 mg iv over 3-5 min. 15-30 min prior to induction.

66
Q

Periop reglan
Dose after delivery
Dose kids post t+a PACU
Dose pre induction w diabetic gastroparesis

A

0.15 mg/kg iv
0.15 mg/kg
10 mg

67
Q

Reglan SE

A 
Cramping if given in less than 3 min 
Cardiac dysrhythmias esp w zofran 
Sedation, dry mouth, EPS (Torric) 
Inc sedation of butyrophenones and phenothiazines 
May inhib cholinesterase
68
Q

Reglan contraindications 4

A

Bowel obstruction
Parkinson’s disease
Seizure disorders
In combo w phenothiazines

69
Q

5ht
Where 90% lives
10%
Drugs that antagonize here

A

Enterochromaffin cells in gut
CNS and plt
TCAs and phenothiazines

70
Q

Ondanzetron

MOA

A

5ht3 antag. Selective antagonism at peripheral (vagal afferrent gi) and central receptors

71
Q

5ht3 antag

Useful in which 3 settings

A

Chemo
Postop NV
Hyperemesis gravidarium

72
Q

SE 5HT3 antag

Careful w what disease

A

HA w rapid admin
Cardiac dysrhythmias rare
Rely on liver metab, reduce in renal disease

73
Q

PONV dosing
Zofran
Adults
Peds

A

4-8 mg iv

0.05-0.15 mg/kg (up to 4 mg)

74
Q

PONV dosing
Granisetron
Dolasetron

A

G- 0.01-0.04 mg/kg

D- 12.5 mg iv adults

75
Q

Steroids to prevent ponv/dose

A

Dexamethasone

4-10 mg iv

76
Q

Phenothiazines

2 ex, how they work

A

Compazine and phenergan. Interact w dopaminergic receptors in Crtz

77
Q

Phenergan
Onset iv
Use 4

A

5 min

Blood trans rxn, allergic rxn, sedation, PONV

78
Q 
Phenergan 
Duration 
1/2 life 
Metabolism 
Contra
A

4-6hrs
9-16 hrs
Liver
Under 2 y/o (fatal resp depression/comatose states)

79
Q

Neuroleptic malig syndrome

Occurs w what, when

A

0.5-1% rx phenothiazines. 24-72hrs, young men

80
Q

Neuroleptic malig syndrome

Presentation

A

Tachy/dysrhythmias, alt bp, fluc LOC. Sim to MH W: muscle rigidity, high temp, rhabdo, autonomic instability

81
Q

Neuroleptic syndrome
Tx
How diff from MH

A 
Dopamine antag (amantadine) and dantrolene 
NDMR will produce rapid paralysis in NMS but not MH
82
Q

Butyrephonones
Which one
MOA
Dose

A

Droperidol
Inhib dopaminergic receptors in crtz
0.625-1.25 mg IV for PONV

83
Q

Droperidol
Effects
Use
Now what, why

A

Dec bp central effect, peripheral alpha blockade, EPS, akathesia, dysphagia
Neuroleptic anesthesia
Block box bc of torsades

Pharmacology (19 decks)

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