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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
H2 antagonists MOA 4 agents
Competitive antagonist at h2 receptor, suppresses gastric acid sec by parietal cells. Cimetidine, nizatidine, ranitidine, famotidine
26
``` H2 antagonists Decreases intracellular __ Least potent Most potent No effect where ```
CAMP Cimetidine Famotidine LES tone/gastric emptying
27
H2 antag work on which pump
H K atpase
28
H2 antagonists effects
Tx duodenal ulcers and gerd, chemoprophylaxis prior to induction of GA
29
Chemoprophylaxis doses/when to give | Cimetidine
300 mg po/iv 1-2hrs preop
30
Chemoprophylaxis doses/when to give | Famotidine
20-40 mg po/20 mg iv am of surgery
31
Chemoprophylaxis doses/when to give | Ranitidine
150 mg po or 50 mg iv
32
H2 antagonists | No effect where
No effect on gastric pH. Unpredictable volume effect
33
H2 antagonists Metab Cmax
Rapid oral abs, 1st pass metab, 50% bioavailability | 1-3 hrs
34
H2 antagonists Protein binding BBB Elim
15-35% All 4 cross it 1.5-4 hrs
35
H2 antagonists Which one renal exc Metabolism primarily
Nizatidine | Other 3 hepatic metab
36
H2 antag SE Which 2 things inc SE severity May have transient elev of
Multisystem disease and inc age | LFTs
37
H2 Antagonists Avoid rapid admin of __ and __, why Give over what time period
Cimetidine and ranitidine Hypotension and bradycardia 15-30 min
38
H2 antagonists | __ may be given over 2 min
Famotidine
39
H2 antagonists | Decreases metab of what
Drugs w hepatic metab. Propranolol and diazepam
40
H2 antagonists | Cimetidine may slow metab of __ and other __
Lidocaine, drugs
41
Goals of PUD therapy 3
Reduce gastric acidity, enhance mucosa, elim h pylori
42
Drug tx PUD For acid Mucosa H pylori
H2 antag, PPI, and anticholinergics for acid sec inhib. Antacids to neutralize. Mucosa protection: sucralfate, bismuth, prostaglandins. Abx
43
PPI | Block what
K h ATPase
44
PPI __ absorption Conversion, where
Rapid | Prodrug to active drug in parietal cell canaliculus
45
``` PPI __ bond w proton pump __ half life Metab Crosses __ ```
Covalent Short Cyp 2c19 and 3a4 Crosses placenta
46
PPI | AE
HA, GI disturb, nausea, enteric infections. Long term unknown, maybe carcinoid tumors
47
PPI | Indic for what
PUD w h pylori Hemorrhagic ulcers PUD in pt who req nsaid use
48
Dicyclomine MOA __ effective than h2 antag and PPI AE
Musc ach antag, dec acid sec Less Dry mouth, constip, blurry vision, cardiac arrhythmia, urine ret
49
Where anticholinergics work in parietal cell
Block acetylcholine and Gastrin
50
Sucralfate What it is How it works
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
Sucralfate Doesnt do what Does do what AE
Doesnt alter gastric ph Does relieve symptoms Constip, little systemic absorp, big pills and frequent admin, drug interactions (binds to them)
52
Colloidal bismuth Used in what Protects how
PUD. Coating agent. Protects mucosa from acid and pepsin degradation, forms barrier. Stim mucosal bicarb and prostaglandin, impedes h pylori
53
Prostaglandins Agent Does what AE/contra
Misoprostal, pg analogue. Prevents nsaid induced ulcers. Abd discomfort and diarrhea. Pregnancy
54
Tx h pylori | Triple therapy
Amoxicillin, clarithromycin, PPI
55
H pylori | Quadruple therapy
Tetracycline, metronidazole, PPI, bismuth
56
Antacids | Inc pH to what
5
57
AE of antacids, 4 agents
Constip, diarrhea, electrolyte abn | Al oh, mg oh, na hco3, ca co3
58
``` Na citrate/bicitra What kind of antacid Onset Dose PH ```
No particulate, clear 15-30 min to facial mixing and emptying 15-30 ml po 8.4
59
Reglan MOA __ only, __ unchanged
Dopamine antagonist | Kinetic, pH
60
Reglan | What it does to GI tract 3
Cholinergic stim. Inc LES tone, inc gastric/small bowel motility, relaxes pylorus and duodenum
61
Reglan Post synaptic release of __ Opposed by what
Ach. Atropine and glyco
62
Reglan ___ effects Stim __ secretion __ __ effects
CNS effects, EPS Prolactin Anti emetic
63
``` Reglan Absorption Peak E 1/2 Excretion ```
Rapid po 40-120 min 2-4 hrs Renal exc, 40% unchanged
64
Reglan uses | 4
Dec gastric fluid vol Antiemetic Gastroparesis Gerd symptomatic tx
65
Reglan periop | When/how to give before induction
10-20 mg iv over 3-5 min. 15-30 min prior to induction.
66
Periop reglan Dose after delivery Dose kids post t+a PACU Dose pre induction w diabetic gastroparesis
0.15 mg/kg iv 0.15 mg/kg 10 mg
67
Reglan SE
``` 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
Reglan contraindications 4
Bowel obstruction Parkinson's disease Seizure disorders In combo w phenothiazines
69
5ht Where 90% lives 10% Drugs that antagonize here
Enterochromaffin cells in gut CNS and plt TCAs and phenothiazines
70
Ondanzetron | MOA
5ht3 antag. Selective antagonism at peripheral (vagal afferrent gi) and central receptors
71
5ht3 antag | Useful in which 3 settings
Chemo Postop NV Hyperemesis gravidarium
72
SE 5HT3 antag | Careful w what disease
HA w rapid admin Cardiac dysrhythmias rare Rely on liver metab, reduce in renal disease
73
PONV dosing Zofran Adults Peds
4-8 mg iv | 0.05-0.15 mg/kg (up to 4 mg)
74
PONV dosing Granisetron Dolasetron
G- 0.01-0.04 mg/kg | D- 12.5 mg iv adults
75
Steroids to prevent ponv/dose
Dexamethasone | 4-10 mg iv
76
Phenothiazines | 2 ex, how they work
Compazine and phenergan. Interact w dopaminergic receptors in Crtz
77
Phenergan Onset iv Use 4
5 min | Blood trans rxn, allergic rxn, sedation, PONV
78
``` Phenergan Duration 1/2 life Metabolism Contra ```
4-6hrs 9-16 hrs Liver Under 2 y/o (fatal resp depression/comatose states)
79
Neuroleptic malig syndrome | Occurs w what, when
0.5-1% rx phenothiazines. 24-72hrs, young men
80
Neuroleptic malig syndrome | Presentation
Tachy/dysrhythmias, alt bp, fluc LOC. Sim to MH W: muscle rigidity, high temp, rhabdo, autonomic instability
81
Neuroleptic syndrome Tx How diff from MH
``` Dopamine antag (amantadine) and dantrolene NDMR will produce rapid paralysis in NMS but not MH ```
82
Butyrephonones Which one MOA Dose
Droperidol Inhib dopaminergic receptors in crtz 0.625-1.25 mg IV for PONV
83
Droperidol Effects Use Now what, why
Dec bp central effect, peripheral alpha blockade, EPS, akathesia, dysphagia Neuroleptic anesthesia Block box bc of torsades

Pharmacology (19 decks)

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