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Pharmacology II > Drugs for Test 2 > Flashcards

Drugs for Test 2 Flashcards

1
Q

Ondansetron (Zofran), Granisetron (Kytril), Dolasetron (Anzemet)- MOA and ROA

A

5-HT3 Antagonists
Antagonism of the 5-HT3 receptor in the chemo-receptor trigger zone
ROA- oral, rectal, IM, IV

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2
Q

Ondansetron (Zofran), Granisetron (Kytril), Dolasetron (Anzemet)- Indications

A

5-HT3 Antagonists
Treatment and prevention of postoperative N/V
Chemotherapy- induced N/V

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3
Q

Ondansetron (Zofran), Granisetron (Kytril), Dolasetron (Anzemet)- ADRs

A

HA
Dizziness
Diarrhea
ABD pain

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4
Q

Metoclopramide (reglan), Trimethobenzamide (tigan), Phenothiazines- Prochlorperazine (compazine), promethazine (phenergen)- MOA

A

Dopamine Antagonists
Antagonist of D2 receptors of the CTZ
At higher doses metoclopramide also blocks 5-HT3 receptors
ALSO PROMOTES GASTRIC EMPTYING AND SMALL INTESTINE PERISTALSIS- PROKINETIC EFFECT

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5
Q

Metoclopramide (reglan), Trimethobenzamide (tigan), Phenothiazines- Prochlorperazine (compazine), promethazine (phenergen)- contraindications

A 
GI- HEMORRHAGE, OBSTRUCTION OR PERFORATION
Cautious use in pts w/ depression
Pheochromocytoma
Seizure
Use w/ caution in children
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6
Q

Metoclopramide (reglan), Trimethobenzamide (tigan), Phenothiazines- Prochlorperazine (compazine), promethazine (phenergen)- ADRs

A

EXTRAPYRAMIDAL EFFECTS
RESTLESSNESS, ANXIETY, DROWSINESS, FATIGUE, HALLUCINATIONS
CV- HTN, HPOTN, AV BLOCK, BRADYCARDIA
AGRANULOCYTOSIS

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7
Q

Promethazine (Phenergen)-MOA

A

Antihistamine
Blocks H1-> effectiness appear to be with motion sickness and vestibulochoclear dz
Antagonist of D2 receptors in the CTZ

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8
Q

Promethazine (Phenergen)- ADRs

A

Dry mouth, dizziness
PARKINSONIAN SYMPTOMS (DYSKINESIA, DYSTONIAS, AKATHISIA)
NEUROLEPTIC MALIGNANT SYNDROME
Blood dyscrasias

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9
Q

Promethazine (Phenergen)- Cautions

A

BPH
Urinary retention
Glaucoma

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10
Q

Dronabinol (Marionol)- MOA and Side effects

A

MOA is not well defined

SE- drowsiness, sedation, increased appetite

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11
Q

Psyllium (metamucil), Methylcellulose (Citrucel), Polycarbophil (Fibercon)- MOA

A

Bulk forming laxatives
Increases the volume of non-absorbable solid residue with water, distending the colon and stimulation peristaltic activity increasing the rate of colonic transit

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12
Q

Psyllium (metamucil), Methylcellulose (Citrucel), Polycarbophil (Fibercon)-Primary Uses and contraindications

A

CONSIDERED 1ST LINE FOR BEDRIDDEN OR GERIATRIC WITH CHRONIC CONSTIPATION, GOOD IN PREGNANCY
Contraindication- pts w/ stenosis, ulceration or adhesions, and fecal obstruction

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13
Q

Psyllium (metamucil), Methylcellulose (Citrucel), Polycarbophil (Fibercon)- ADRs

A

Flatulence
ABD distention
Gastrointestinal obstruction

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14
Q

Psyllium (metamucil), Methylcellulose (Citrucel), Polycarbophil (Fibercon)- drug interactions

A

BINDS DRUGS & REDUCES ABSORPTION- SEPARATE FROM OTHER MEDICATION ADMIN

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15
Q

Psyllium (metamucil), Methylcellulose (Citrucel), Polycarbophil (Fibercon)- other uses

A
  • The ability of these agents to absorb water makes them useful for RELIEVING SX OF MILD DIARRHEA
  • Several months use can RELIEVE SX OF IBS
  • LOWERING CHOLESTEROL
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16
Q

Docusate sodium (Colace)- MOA

A

Emollient
Surfactant brings water into stool, facilitates mixing of aqueous and fatty materials within intestine, increase H20 and electrolyte secretion in small/ large bowel

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17
Q

Docusate sodium (Colace)- uses

A

To avoid straining
After MI, rectal surgery, opiates
1ST LINE PREGNANT WOMEN
Onset 1-3 days

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18
Q

Docusate sodium (Colace)- contraindication

A

Fecal impaction

Signs and sx of appendicitis

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19
Q

Mineral Oil- MOA

A

Lubricant
Coats stool (allows easier passage), inhibits colonic absorption of water
Onset- 6hrs-3 days (oral or rectal)

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20
Q

Mineral Oil- Use and contraindications

A

Used mainly for prevention (to avoid straining and after MI or rectal surgery)
CHRONIC USE IS DISCOURAGES
CAUTION-AVOID IN ELDERLY, ASPIRATION RISK AND DECREASE ABSORPTION OF FAT-SOLUBLE VITAMINS (DEAK)
May leak from anal sphincter

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21
Q

Lactulose- MOA

A

Osmotic agent
Disaccharide that is metabolized by bacteria in the colon to low-molecular weight acids = osmotic effect
Not considered a 1st line therapy

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22
Q

Lactulose- Uses and SE

A

MOST COMMONLY USED IN PTS W/ HEPATIC ENCEPHALOPATHY
Side effects- flatulence, cramps, electrolyte imbalance
Oral dose soften stools in 1-3 days

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23
Q

Sorbital- MOA

A

Osmotic agent
Monosaccharide creates an osmotic gradient when used as a 70% solution
Hyperglycemia
Oral dose soften stool in 1-3 days

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24
Q

Magnesium hydroxide (milk of magnesia), Magnesium sulfate (Epsom salts), Sodium phosphate (fleets enema), Magnesium citrate (citrate of magnesia)- MOA

A

Saline cathartics
Mg++ or Na+ salts are POORLY ABSORBED; THEY INCREASE THE WATER CONTENT OF THE BOWEL THROUGH OSMOSIS
Onset- 30min-6hrs (oral), 5-30min (rectal)

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25
Q

Magnesium hydroxide (milk of magnesia), Magnesium sulfate (Epsom salts), Sodium phosphate (fleets enema), Magnesium citrate (citrate of magnesia)- Contraindications

A

Impaired renal function
Mg and Na accumulation
CHF
No sodium for HTN pts

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26
Q

Caster oil- MOA and use

A

MOA- metabolized to ricinoleic acid (stimulates secretory pathways)
Decreased glucose absorption
Promotes intestinal motility
Not for routine use

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27
Q

Glycerin Suppository- MOA, Use, ADRs

A 
MOA- osmotic action in rectum
Onset <30 min
May cause rectal irritation
Very safe laxative and can be used in children
Intermittent use
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28
Q

Polyethylene Glycol (Miralax)- MOA and use

A

Glycerin/hyperosmotic
MOA- osmotic
Use- 17g mixed in water or juice, usually 2wk duration but chronic is okay
Relatively safe, OK for children

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29
Q

Polyethylene glycol (PEG, GoLYTELY)- MOA

A

Glycerin/hyperosmotic

Osmotoc agent that causes retention of water resulting in softer stool and more frequent defecation

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30
Q

Polyethylene glycol (PEG, GoLYTELY)- USE

A

For COLONIC CLEANSING BEFORE DIAGNOSTIC PROCEDURES

Note- 4 liters over 3 hrs, NOT FOR CHRONIC USE. AVOID IN PTS W/ INTESTINAL OBSTRUCTION

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31
Q

Bisacodyl (Dulcolax) MOA

A

Stimulant laxative
Diphenylmethane derivative
Stimulate nerve plexus of the colon
onset 6-8 hrs PO; 1-6 hrs PR

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32
Q

Bisacodyl (Dulcolax)- Contraindications and ADRs

A

SHOULD NOT TAKE W/IN 1 HR OF ANTACIDS, MILK OR MILK PRODUCTS
Intestinal cramping
CAN CAUSE FLUID AND ELECTROLYTE INBALANCE
PINK COLORED URINE AND FECES
Long term use- could cause damage to the nerve plexi resulting in deterioration of intestinal function
ATONIC COLON

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33
Q

Senna (Senokot)- MOA

A

Stimulant laxative
Anthraquinone laxative
MOA- increased peristalsis

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34
Q

Senna (Senokot)- ADRs

A

YELLOW-BROWN TO RED COLORED URINE
LARGE DOSES CAN PRODUCE NEPHRITIS
Long term use- CAN CAUSE DAMAGE TO THE NERVE PLEXI (resulting in deterioration of intestinal funciton), STONIC COLON

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35
Q

Senna (Senokot)- contraindications

A

Contraindications- PREGNANCY AND ACUTE INTESTINAL INFLAMMATION

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36
Q

Lubiprostone (Amitiza)- MOA

A

Chloride-channel activator…works by increasing fluid secretion locally in the small intestine by activating the ClC-2 chloride channel

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37
Q

Lubiprostone (Amitiza)- Side effects and contraindications

A

Side effects- nausea and diarrhea

Contraindications- INTESTINAL OBSTRUCTION AND PREGNANCY

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38
Q

Methylnaltrexone- MOA

A

Peripherally acting antagonist of mu
Expensive
Does not cross the blood brain barrier
Reduced the effects of opioids peripherally (not centerally)

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39
Q

Opiates and Derivates, Loperamide, Diphenoxylate, Paregoric, Difenoxin- MOA

A

Antimotility
Slow intestinal transit
Prolong contact and absorption
Increase gut capacity

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40
Q

Opiates and Derivates, Loperamide, Diphenoxylate, Paregoric, Difenoxin- Caution

A

Addiction potential

Worsen diarrhea if infectious

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41
Q

Lomotil- Onset and Contraindications

A

Clinical benefit usually w/in 48 hrs
If no benefit in 10 days, change therapy
Contraindications- C. diff or entertoxin

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42
Q

Loperamide (Imodium)- MOA

A

Acts directly on intestinal muscles to inhibit peristalsis, prolonging transit time

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43
Q

Loperamide (Imodium)- Onset and contraindication

A

Clinical benefit usually w/in 48 hrs
Contraindications- Pts w/ a fever exceeding 101 F (38.3c), acute ulcerative colitis, ABX associated colitis, and children under 2

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44
Q

Kaolin-pectin, polycarbophil, attapulgite- MOA

A

Adsorbents
Absorb nutrients, toxins, drugs, and digestive juices
Effectiveness unproven in trials, many do not require RX.

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45
Q

Cholestryamine (Questran)- MOA

A

Absorbs bile salts and C. diff toxin

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46
Q

Pepto-Bismol-MOA and Onset

A

Bismuth subsalicylate
Stimulates absorption of fluid and electrolytes across the intestinal wall
Onset- <48 hrs

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47
Q

Pepto-Bismol- Side effects

A

Not for kids Reyes syndrome
Blackened stool and tongue
Salicylism
Can induce gout attacks

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48
Q

Pepto-Bismol- Interactions

A

Anticoagulants and tetracycline; May interfere with radiologic studies

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49
Q

Octreotide (Sandostatin)- MOA

A

Antisecretory
Blocks the release of serotonin, direct inhibitory effects
Reduces motility and facilitates water absorption from the gut

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50
Q

Octreotide (Sandostatin)- Use and onse

A

Official indication- control sx in pts with metastic vasoactive intestinal peptide-secreting tumor associated diarrhea
Off labe use- tx of refractory diarrhea
Onset- 1-3 days up to a week

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51
Q

Octreotide (Sandostatin)- ADRs

A

BRADYCARDIA

HYPERGLYCEMIA

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52
Q

Atropine- MOA

A

Anticholinergic

Blocks vagal tone and prolongs gut transit time

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53
Q

Atropine- ADRs and contraindications

A

ADR-anticholinergic side effects

Contraindicated- glaucoma, prostatic hypertrophy

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54
Q

Lactobacillus-MOA

A

Bacterial replacement

Restores normal flora and intestinal function

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55
Q

Lactobacillus- ADRs and contraindications

A

Intestinal flatus

Contraindicated in immuno-compromised patients

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56
Q

Lactase Enzymes-MOA and Use

A

MOA- replaces lactase enzyme deficiency

Use- only useful in lactose intolerance

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57
Q

Zinc

A

Substantial data supporting zinc in diarrhea as adjunct to ORS
Reduction of Stool output
Reduction of diarrhea duration
MOA is unknown, possibly action on intestinal ion transport

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58
Q

Antacids- MOA

A 
Neutralize acid to raise intragastric pH
Decrease activation of pepsinogen
Increased LES pressure
Benefit- rapid onset
Disadvantage- short duration
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59
Q

Antacid- Side effects

A 
GI- diarrhea or constipiation
- diarrhea: magnesium
-constipation: aluminum
-Gas: calcium, sodium bicarbonate
Sodium bicarbonate products can cause fluid overload in pts. with CHF, renal failure, cirrhosis, pregnancy, or any salt-restricted diet; avoid in anyone taking supplemental calcium or with renal dysfunction
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60
Q

Antacid- Drug interactions

A

alter gastric pH, increase urinary pH, adsorbing medications, physical barrier to absorption, form insoluble complexes
Clinically significant- abx- quinolone, isoniazid, tetracycline, ferrous sulfate, quinidine, sulfonylurea

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61
Q

Antacids- Precautions

A

Use of med >14 days needs evaluation for barrett’s esophagus and upper GI pathology due to increased risk
Pts excessively using antacids should be treated w/ rx drugs, and is considered more significant disease.

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62
Q

H2 receptor antagonists- MOA

A

Reversibly inhibit histamine-2 receptors on parietal cells

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63
Q

H2 receptor antagonists- USE

A

On-demand therapy for intermittent mild to moderate GERD symptoms
Preventive dosing before exercise/meals
Prescription strengths needed for more severe symptoms or for maintenance dosing
Less effective than PPIs in healing erosive esophagitis

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64
Q

What drugs are H2 receptor antagonists?

A 
Ranitidine (Zantac)
Cimetidine (tagamet)
Nixatidine (Axid)
Famotidine (Pepcid)
Pepcid Complete
These resemble histamines
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65
Q

H2- receptor antagonist- Absorption, fate, and excretion

A

H2 receptor antagonists are rapidly & well absorbed after oral admin.
Peak conc. 1-2 hours
Oral bioavailability of nizatidine ~ 90%
-Whereas first-pass metabolism limits bioavailability of the other compounds to ~50%,
A large part of these drugs are excreted unchanged in the urine and therefore may need a reduction in dosage w/renal impairment.

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66
Q

H2- receptor antagonist- side effects

A

Well tolerated
HA, somnolence, fatigue, dizziness, constipation or diarrhea
Thrombocytopenia: rare, reversible

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67
Q

H2- receptor antagonist- Drug interactions

A

Cimetidine
-Inhibition of metabolism of warfarin, phenytoin, nifedipine, propranolol
Acidic environment required for absorption
-Ketoconazole, itraconazole, ferrous sulfate

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68
Q

Antacids vs H2-receptor antagonist

A

Combination more effective than antacid therapy alone

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69
Q

What are the names of the PPIs?

A

Prototypes- omeprazole (prilosec)

Other agents- Lansoprazole (prevacid), esomeprazole (nexium), pantoprazole (Protonix), rabeprazole (aciphex)

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70
Q

Proton pump inhibitor- MOA

A
  • Inhibit the action of the H+,K+ -ATPase.
  • All considered prodrugs in that they need to be activated to be effective. They need the acidic environment (H+) to work.
  • Requires 18 hours to synthesize new H+,K+ -ATPase molecules
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71
Q

Proton pump inhibitor- ADRs

A

Generally uncommon
N/D/C
HA, dizziness, somnolence
May have higher incidence of community-acquired pneumonia
-Clinical significance unclear
-Pts with asthma, COPD, immunocompromised, young or elderly may be at risk

72
Q

Proton pump inhibitors- Drug interactions

A

P450s
Omeprazole, lansoprazole, esomeprazole and pantoprazole metabolized by P450 enzymes (rabeprazole metabolized thru nonenzymatic reduction pathway)
Omeprazole and esomeprazole reduce metabolism of: Diazepam, Phenytoin, warfarin

73
Q

Promotility agents- Side effects

A

Limited side effect profile:
CNS effects: drowsiness, irritability, extrapyramidal effects
–Metoclopramide (Reglan): contraindicated in Parkinson’s Dz, mechanical obstruction, concomitant use of other dopamine antagonists, anticholinergics, and pheochromocytoma
–Bethanechol (Urecholine): may increase acid production, not well tolerated due to cholinergic side-effects (usually used for the bladder and not intestines)
–Fatal cardiac dysrhythmia: cisapride

74
Q

Sulcralfate- MOA

A

Mucosal protectant
Non-absorbable aluminum salt
Compared to H2-receptor antagonist for mild esophagitis
Less effective in refractory esophagitis

75
Q

Sulcralfate (Carafate)- Chemistry and effects

A
  • When the pH is below 4, an extensive polymerization & cross-linking of sucralfate to form a sticky, viscid, yellow-white gel.
  • The gel adheres to epithelial cells and adheres very strongly to the base of ulcer craters.
76
Q

Sulcralfate (Carafate)- Clinical utility

A
  • Effective at promoting healing in PUD
  • As a maintenance therapy–more efficacious in duodenal than gastric ulcers.
  • Used to prevent stress ulcers
  • More effective when administer prior to meals than after since acid is needed for activation.
77
Q

Sulcralfate (Carafate)- ADRs

A

Constipation - A3+
Dry mouth
Abdominal discomfort

78
Q

Sulcralfate (Carafate)- drug interactions

A

Phenytoin
Tetracycline
Fluroquinolone Antibiotics
Digoxin
Ketocanazole
Better to administer these meds 2 hrs before sucralfate
DO NOT administer w/ agents that decrease acid

79
Q

What is the three drug regimen for peptic ulcer dz?

A 
P= PPI
A= Amoxicillin
C= Clarithromycin

OR

P=PPI
M==Metronidazole
C=Clarithromycin

80
Q

what is the drug of choice for PUD?

A

PPIs

81
Q

What is the 4 drug regimen for peptic ulcer dz?

A

P=PPI (or H2 blcoker)
B= Peto bismol
M=Metronidazole
T=tetracycline (or amox, or clarithro)

82
Q

Bismuth Subsalicylate (pepto-bismol)- beneficial effects

A

Cytoprotection through enhanced secretion of mucus and HCO3-.
Inhibit pepsin activity.
Accumulate bismuth subcitrate in craters of gastric ulcers.
Antibacterial effects: Reduce bacterial adherence to mucosal cells, Damage bacterial cell walls.
Promote healing of both gastric and duodenal ulcers

83
Q

Bismuth Subsalicylate (pepto-bismol)- ADRs

A
  • Reaction of bismuth w/bacterial H2S leads to bismuth sulfide causing a black color to the oral cavity and to feces.
  • Aspirin ADRs
84
Q

Prostaglandin Analogs- MOA

A
  • Misoprostol is a synthetic analogue of prostaglandin E.
  • Imitates the action of endogenous prostaglandins (PGE2 and PGI2) in maintaining the integrity of the gastroduodenal mucosal barrier.
  • Promotes healing.
85
Q

Prostaglandin analogs- Indications

A

Ulcer healing

Ulcer prophylaxis w/ NSAID use

86
Q

Prostaglandin Analog- contraindications

A

Hypotension
Breastfeeding
Pregnant

87
Q

Prostaglandin Angalog- ADRs

A

Diarrhea

Constipation

88
Q

Inhaled corticosteroids-MOA

A

Depress the inflammatory response and edema in the respiratory tract and diminish bronchial hyper-responsiveness.

  • -Reduced mucous production
  • -Decreased local generation of prostaglandins and leukotrienes, with less inflammatory cell activation (decreased inflammation)
  • -Adrenoceptor up-regulation
  • -Long-term reduced eosinophil and mast-cell infiltration of bronchial mucosa.
89
Q

Inhaled corticosteroids- ROA

A

Metered dose inhaler
Oral
IV for severe asthma attack

90
Q

Inhaled corticosteroids- Indications

A
  • Most EFFECTIVE long-term control therapy for persistent asthma
  • Only therapy shown to reduce the risk of death from asthma even in low doses
  • Often used in combination with β2 agonist or other asthma agents.
91
Q

Inhaled corticosteroids- response to therapy?

A
  • Symptoms improve in 1-2 weeks; max in 4-8 weeks
  • FEV1 and peak expiratory flow require 3-6 weeks for max improvement
  • BHR improvement in 2-3 weeks; max 1-3 months
  • *Note- inhaled corticosteroids must be used regularly to be effective.
92
Q

Inhaled corticosteroids- contraindications and ADRs

A

Contraindication- caution in growing children
ADRS:

Local
Oropharyngeal candidiasis (Thrush)
Dysphonia
Reflex cough and bronchospasm

Potential systemic effects- not seen if low regular doses are being used
Hypothalamic-pituitary-adrenal suppression
Impaired growth in children
Dermal thinning-Dose Dependant
Osteoporosis and glaucoma

93
Q

Inhaled corticosteroids- Adverse effects in adults

A

Bone mineral density
–Data suggest cumulative dose relationship
If risk for osteoporosis consider bone-protecting therapy
Ocular effects
–High cumulative lifetime exposure may increase prevalence of cataracts
–Increase risk of glaucoma if family history

94
Q

How can you reduce the potential for adverse effects in inhaled corticosteroids?

A
  • Using a holding chamber (spacer)
  • Rinse mouth (rinse and spit) after inhaler use
  • Using lowest dose possible- if controlled on low dose don’t give them medium or high dose
  • Using in combination with long-acting beta2-agonists (LABA)
95
Q

What are the medication names of inhaled corticosteroids?

A 
Fluticasone (Flovent, Flovent Diskus)
Budesonide (Pulmicort Flexhaler, Pulmicort Respules)
Beclomethasone HFA (Ovar)
Flunisolide (Aerobid, aerobid-M)
Triamcinolone (Azmacort)
Mometasone (Asmenex)
Ciclesonide (Alvesco)
96
Q

What are the ICS and LABA combinations?

A

Fluticasone/salmeterol (Advair Diskus, Advair HFA)

Budesonide/formoterol (Symbicort HFA)

97
Q

What are the long acting beta2 agonists (LABAs)?

A 
Salmeterol (Serevent)
Formoterol (Foradil)
Fluticasone/salmeterol (advair)
Budesonide/formoterol (symbicort)
Arformoterol tartrate (Brovana)
Formoterol fumerate (Perforomist)
98
Q

LABA’s use

A

Not a substitute for anti-inflammatory therapy
Not appropriate for monotherapy
Beneficial when added to inhaled corticosteroids
Not for acute symptoms or exacerbations
–20 minutes for onset (salmeterol)- that’s too late

99
Q

LABAs

A

Tolerance with chronic administration
Partial loss of protective effect against- Methacholine, Histamine, Exercise
Bronchodilator response not decreased
Responsiveness to SABA slightly decreased

100
Q

What is the black box warning associated with Long acting beta 2 agonists (LABA)?

A

May increase the change of severe asthma episodes, and death when those episodes occur

Trying to get rid of this not entirely accurate.
Taking this drug in combo with a steroid DECREASES risk of death but taking it alone could increase asthma and death.

101
Q

LABA- interactions

A
  • Concomitant use of CYP3A4 inhibitors increase salmeterol plasma levels
  • Avoid: Ketoconazole, ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, saquinavir, telithromycin
  • -Prolonged QTc intervals
  • -Palpitations
  • -Tachycardia
102
Q

What are the Leukotriene receptor antagonists?

A

Montelukast (Singulair)
Zafirlukast (Accolate)
Zileuton (Zyflo)

103
Q

Montelukast (Singulair), Zafirlukast (Accolate),

Zileuton (Zyflo)- MOA

A

–Competitively antagonize leukotriene receptors D4 and E4 in the bronchiolar muscle, antagonizing endogenous leukotrienes causing bronchodilation.

Zileuton inhibits 5-lipoxygenase—an enzyme necessary for leukotriene synthesis.

Endogenous leukotrienes are thought to cause airway narrowing which is sometimes seen with the use of NSAIDs.

104
Q

Montelukast (Singulair), Zafirlukast (Accolate),

Zileuton (Zyflo)- ROA and indications

A

Oral

Alternative tx of mild persistant asthma

105
Q

Montelukast (Singulair), Zafirlukast (Accolate),

Zileuton (Zyflo)- Contraindications

A

Pregnancy
Caution in elderly
Zileuton is contraindicated in patients with active liver disease

106
Q

Montelukast (Singulair), Zafirlukast (Accolate),

Zileuton (Zyflo)- ADRs

A

GI disturbances (stomach pain, heartburn)
HA
Zileuton and Zafirlukast liver toxicity
Zafirlukast and montelukast can increases respiratory infections in elderly patients

107
Q

Montelukast (Singulair), Zafirlukast (Accolate),

Zileuton (Zyflo)- drug interactions

A

Zafirlukast
Interaction with Warfarin – increase in prothrombin time (~35%)
Food can reduce bioavailability
Take 1 hour before or 2 hours after meals

Zileuton
Theophylline – doubles theophylline concentration
Warfarin – increase prothrombin time
Propranolol- doubles propranolol AUC

108
Q

What are the methylxanthine drugs?

A

Theophyllline (Theo-24, Theochron, Theolair)

Aminophylline

109
Q

Theophyllline (Theo-24, Theochron, Theolair)

Aminophylline- MOA

A

Methylxanthine
Appear to increase cAMP levels in the bronchial smooth muscle cells by inhibiting phosphodiesterase, an enzyme which catalyses the hydrolysis of cAMP to AMP. Increased cAMP relaxes smooth muscle, causing bronchodilation

110
Q

Theophyllline (Theo-24, Theochron, Theolair)

Aminophylline- Route and indications

A

Oral
Aminophylline-IV in severe asthma attacks

Use- refractory patients and used as monotherapy and combination therapy w/ ICS

111
Q

Theophyllline (Theo-24, Theochron, Theolair)

Aminophylline- Contraindications

A

Not recommended in children < 4 years
Cardiac disease
HTN
Hepatic impairment

112
Q

Theophyllline (Theo-24, Theochron, Theolair)

Aminophylline- drug interactions

A

–Infrequently used due to narrow therapeutic window, drug-drug interactions and safer alternatives
–Significant drug/disease interactions
Viral illness, CHF, cirrhosis, cigarette smoking,etc
–Significant drug/drug interactions
Cimetidine, macrolides, quinolones, etc
CYP1A2 and 3A4 substrate

113
Q

Theophyllline (Theo-24, Theochron, Theolair)

Aminophylline- adverse effects

A

Nausea, irritability, insomnia, headache, vomiting
–Less frequent when dosing is low and slow

Tachyarrhythmias

Ventricular arrhythmias, seizures

Seizures reported with concentrations of 25 mcg/mL

Minor side effects do not always occur before severe, life-threatening effects

114
Q

What are the mast cell stabilizers?

A 
Cromolyn sodium (intal)
Nedocromil (tilade)
115
Q

Cromolyn sodium (intal), Nedocromil (tilade)- MOA and ROA

A

Mast stabalizers
stabilize mast cells preventing the release of inflammatory mediators
Route- Inhaled

116
Q

Cromolyn sodium (intal), Nedocromil (tilade)- Indications

A

Patients pregnancy

117
Q

Cromolyn sodium (intal), Nedocromil (tilade)- ADRs

A 
Mast stabalizers
Cough 
Transient bronchospasm
Throat irritation
Neocromil has a bitter taste
Note: Must be utilized regularly for several weeks before effects are noted.  Not indicated for acute asthma.
118
Q

Omalizumab (Xolair)- MOA

A

Immunomodulator
Recombinant monoclonal antibody that binds IgE on mast cells and basophils limits release of mediators of allergic response

119
Q

Omalizumab (Xolair)- indications

A

For moderate-to-severe persistent asthma in patients 12 years of age or older who are not controlled on other therapies (not first line therapy Reserved )

120
Q

Omalizumab (Xolair)- Safety profile

A 
Black Box Warning for anaphylaxis
Anaphylaxis in 0.1% of patients
May develop after any dose
70% of reactions within 2 hours
May be delayed up to 24 hours
Cost-effectiveness and long-term efficacy unknown at this time
121
Q

Systemic corticosteroids-MOA

A

Decrease inflammation by suppression of migration of leukocytes and reversal of increased capillary permeability.

122
Q

Systemic corticosteroids- indications and ROA

A

Control chronic symptoms in people with severe asthma
Can be used for maintenence but mainly used for acute asthma
Oral therapy preferred over IV

123
Q

What are the quick relief treatments for asthma?

A

Bronchodilators
–Short Acting Beta2-adrenoceptor agonist
Albuterol: Ventolin® HFA, Proventil® HFA, Proair® HFA- DOC
Pirbuterol: Maxair®
Metaproterenol
Levalbuterol: Xopenex®- r enantimer of albuterol

124
Q

Beta2-adrenoceptor agonist- MOA

A
  • β2-adrenoceptors are located on the airway smooth muscles and respond to epinephrine.
  • Stimulation of β2-adrenoceptors leads to a rise in intracellular cAMP levels and subsequent smooth muscle relaxation and bronchodilation.
  • β2-adrenoceptor agonist may also prevent activation of mast cells as a minor effect
  • β2-adrenoceptor agonist are potent bronchodilators with little if any β1 stimulating properties.
125
Q

Beta2-adrenoceptor agonist- Indications

A

Relieve bronchospasm during acute exacerbations
Pretreatment for exercise induced bronchoconstriction
Treat the symptoms of asthma but not the underlying disease.
Does not improve control of symptoms
Alone in mild asthma
Adjunct to corticosteroids

126
Q

Beta2-adrenoceptor agonist- ADRs

A

Fine tremor
Tachycardia
Hypokalemia w/ high doses- albuterol encourages potassium to go intracellulary
Some patients have increased risk of exacerbations, some have decreased lung function
Does not appear to occur with prn use
Short-acting beta agonist such as albuterol are the only inhaled agents indicated for acute asthma attacks therefore also used as rescue inhalers.

127
Q

What are the anticholinergic (Antimuscarinics)?

A

Ipratropium (Atrovent)

Tiotropium (Spiriva, Handihaler)

128
Q

Anticholinergics- Ipratropium (Atrovent), Tiotropium (Spiriva, Handihaler)- indications

A
  • Relief of acute bronchospasm
  • Not indicated for chronic therapy
  • Ipratropium may provide additive effects to B2-agonists, in acute setting
  • Alternative for patients with B2-agonist intolerance
  • Treatment of choice for bronchospasm due to B-blockers
129
Q

Anticholinergics- Ipratropium (Atrovent), Tiotropium (Spiriva, Handihaler)- MOA

A

Parasympathetic vagal fibers provide a bronchoconstrictor tone to the smooth muscle of the airways. Activated by reflex with stimulation of sensory receptors in the airway walls.
Muscarinic antagonists act by blocking muscarinic receptors, especially M3 subtype, which responds to this parasympathetic brochoconstrictor tone.

130
Q

Anticholinergics- Ipratropium (Atrovent), Tiotropium (Spiriva, Handihaler)- Contraindications

A

Glaucoma

Pregnancy

131
Q

Systemic Corticosteroids- Indication

A
  • -Important in the treatment of severe acute exacerbations
  • -Prevent progression of asthma exacerbation
  • -Reduce need for referral to ER and hospitalization
  • -Prevent early relapse after emergency treatment
  • -Reduce morbidity of the illness
  • -More than three courses/year → re-evaluate asthma management plan
132
Q

Oxygen

A

Administered to any patient in respiratory distress except COPD patients who retain CO2. Caution should be used in these patients not to administer too much O2 to depress their respiratory drive.
It increases alveolar oxygen tension and decreases the work of breathing necessary to maintain arterial oxygen tension.

133
Q

What are the aminosalicylate drugs?

A

Sulfasalazine

Mesalamine

134
Q

Sulfasalazine (Azulfidine)-MOA

A

Aminosalicylate

Metabolized by intestinal bacteria to to the active component 5-aminosalicylate (5-ASA) and sulfapyridine (mesalamine)

135
Q

Sulfasalazine (Azulfidine)- use

A

Most commonly used for inducing and maintaining remission

Response can take 2-3 weeks

136
Q

Sulfasalazine (Azulfidine)- contraindications

A

SALICYLATE HYPERSENSITIVITY

Renal impairment- monitor SCr

137
Q

Sulfasalazine (Azulfidine)- side effects

A

NOT WELL TOLERATED
N/V, heartburn, anorexia
HA
HYPERSENSITIVITY RXNS (RASH, FEVER)- DO NOT USE IN PTS W/ SULFA ALLERGY
BLOOD DISORDERS (ANEMIA, THROMBOCYTOPENIA, GRANULOCYTOPENIA)
CAN IMPAIR FOLIC ACID ABSORPTION
IDIOSUNCRATIC RXNS (HEPATOCELLULAR INJURY, AGRANULOCYTOSIS, LUPUS-LIKE SYNDROME)
LOW SPERM COUNTS

138
Q

Mesalamine (Asacol, Rowasa, Pentasa, Canasa)- MOA

A

Aminosalicylate
Unclear various effects on inflammatory process
Formulations vary and target different parts of the colon
Mesalamine or suppositories for rectosigmoid disease
Delayed release formulations of mesalamine for Crohn’s ileitis
Response is slow

139
Q

Mesalamine (Asacol, Rowasa, Pentasa, Canasa)- side effects

A

Local itching and mild rectal irritation with topical enemas

Idiosyncratic rxns: pleuropericarditis, pancreatitis, nephrotic syndrome

140
Q

What are the corticosteroids?

A

Prednisone, Budesonide, Prednisolone, Hydrocortisone, Methyprednisolone (available in a syrup)

141
Q

Corticosteroids- MOA

A

Anti-inflammatory effects
Improves Symptoms
Improves disease severity

142
Q

Corticosteroids-ROA

A

PO
IV- hospitalization for parenteral
Topical: suppositories, foams, enemas (effective in distal colonic inflammation)

143
Q

Corticosteroids- tapering

A

Induction of response takes 7-14 days
Taper by 5mg/wk prednisone or equivalent
Budesonide taper: 9mg6mg3mg
Inability to taper is indication for amtimetabolite and/or infliximab therapy
Parenteral steroid indicated in pts failing to respond to 7-14 days of high dose oral prednisone or equivalent

144
Q

Corticosteroids- monitoring for complications

A

Glucose intolerance/ metabolic abnormalities
Hyperkalemia
Hyponatremia
glucose

Greater risk for adrenal insufficiency and infections
N/V
Postural hypotension

Long-term therapy (>3mo)
Bone density
Annual eye exam

145
Q

What are the immunosuppressives?

A

6-Mercaptopurine (6-MP)

Azathioprine (Imuran)

146
Q

What is azathiprine (imuran)?

A

A prodrug metabolized to 6-MP

147
Q

Immunosuppressives- 6-Mercaptopurine (6-MP), Azathioprine (Imuran)- MOA

A

Antagonizes purine metabolism; inhibits DNA, RNA and protein synthesis
Steroid-sparing achieve or maintain control and allow reduction or discontinuation of steroids

148
Q

Immunosuppressives- 6-Mercaptopurine (6-MP), Azathioprine (Imuran)- Toxicity bone marrow and pancreas5

A 
Bone marrow suppression 2-5%
Dose related
Managed by dose reduction/withdrawal
Leukopenia, thrombocytopenia, pancytopenia
RISK OF LYMPHOMA 4 FOLD INCREASE

Pancreatitis 1.3-3.3%
Dose independent
Occurs within 3-4 weeks of start
Resolves with stopping drug

149
Q

Immunosuppressives- 6-Mercaptopurine (6-MP), Azathioprine (Imuran)- Toxicity GI effects, others, and Infections

A

GI effects
N/V, abdominal pain
Occurs early, improves with time or with dose reduction

Other
Fever, rash, arthralgias
Dose independent

Infections
Disseminated CMV, herpes zoster, pneumonia, Q fever, viral hepatitis
Occur without leukopenia
Increased risk if combined with steroids

150
Q

Immunosuppressives- 6-Mercaptopurine (6-MP), Azathioprine (Imuran)- drug interactions

A 
Inhibition of metabolism leading to increased myelosuppression
Sulfasalazine, mesalamine
Allopurinol
Aspirin
Furosemide
151
Q

What is the immunodulator drug?

A

Methotrexate

152
Q

Immunodulator- Methotrexate- MOA

A

Folic acid antagonist with anti-inflammatory effects
Reduces steroid needs
Improves disease control

153
Q

Immunodulator- Methotrexate- ADRs

A

Nausea

Elevated transaminases- huge problem have to monitor for LFT

154
Q

Immunodulator- Methotrexate- Toxicities

A

Leukopenia
N/V
Absolute contraindication in pregnancy (Category X)
–Stop therapy 3 months prior to conception
–Folate supplementation prior to conception
–Contraindicated in breastfeeding
Hypersensitivity pneumonitis (rare)
Hepatic fibrosis
–Most significant in long term therapy
–Risk with >1500 mg total cumulative dose and daily dosing
–DC if moderate/severe fibrosis or cirrhosis found on biopsy

155
Q

Cyclosporin (Neoral or Sandimmune)-MOA

A

MOA: inhibits production and release of IL-2  inhibits activation of T-lymphocytes

Concomitant IV steroids recommended

Cyclosporin alone unable to maintain remission
Requires “bridging” with AZA or 6-MP
Convert IV to PO
PO dose is 2x IV dose
Wean off cyclosporin and steroids over next few months

156
Q

Cyclosporin (Neoral or Sandimmune)- toxicities

A 
HTN
Hypertrichosis- abnormal hair growth on the body
ELECTROLYE ABNORMALITIES
NEPHROTOXICITY
Opportunistic Infections
Requires PCP prophylaxis
157
Q

Tacrolimus (Prograf)-MOA

A

inhibits T-lymphocyte activation

Fungus (streptomyces)

158
Q

Tacrolimus (Prograf)- adverse reactions

A 
Tend to resolve with dose reductions
HA
Increased serum creatinine
Nausea
Insomnia
Leg cramps
Paresthesias
Tremors
159
Q

What are the monoclonal antibodies?

A

Infliximab (Remicade)
Adalimumab (Humira)
Natalizumab (tysabri)

160
Q

Infliximab (remicade)- MOA

A

Monoclonal Antibodies
Monoclonal antibody that binds to TNF-alpha
Inhibits inflammatory cytokines, inhibits leukocyte migration and activation of neutrophils

161
Q

Infliximab (remicade)- Contraindications

A 
NYHA class III/IV heart failure
Dose should not exceed 5mg/kg in other pts with congestive heart failure

Hepatitis
Reactivation of hepatitis B
Autoimmune hepatitis
Discontinue use with LFTs 5x ULN

162
Q

Infliximab (remicade)- antibodies to infliximab

A

Increased risk of infusion rxn, shorter duration of response

regularly scheduled less immunogenic than episodic

163
Q

Infliximab (remicade)- Toxicities infections and infusion reactions

A

INFECTIONS
Bacterial, mycosal, mycobacterium
Higher TB rates with more extrapulmonary involvement

INFUSION REACTIONS
During or after (1-2 hrs)
HA, dizziness, nausea, erythema at site, flushing, fever, chills, chest pain, cough, dyspnea, pruritis
Mechanism unclear- not IgE type 1
Doesn’t occur till after 1st infusion; not at every infusion

164
Q

Infliximab (remicade)- Toxicities delayed hypersensitivity, autoantibodies, and malignancy and lymphoproliferative disorder

A

Delayed hypersensitivities
3-14 days after infusion
Myalgia, arthralgia, fever, rash, pruritis, dysphagia, urticaria, HA
Resolve spontaneously or require steroids
Prednisone 40mg PO or methylprednisolone 100mg IV 30 min before
Risk factor: long interval between treatments

Autoantibodies
15-40% develop anti-dsDNA ANA
Development of drug-induced lupus rare
Reversible with DC

Malignancy and lymphoproliferative disorder
Longstanding CD and tx with immunosuppression more likely to develop lymphomas

165
Q

Adalimumab (Humira)- MOA

A

recombinant fully-human immunoglobulin-1 anti-tumor necrosis factor (TNF)-alpha monoclonal antibody
Evaluate for TB before starting therapy

166
Q

Adalimumab (Humira)- Side effects

A

BLACK Box Warning of serious infections
TB, invasive fungal, other opportunistic infections

Rash, injection site rxn, HA, URI, development of autoantibodies to drug, development of anti-nuclear antibodies (ANA)

Risk of reactivating hepatitis B

167
Q

Natalizumab (tysabri)- MOA

A

recombinant immunoglobulin-4 monoclonal antibody

168
Q

Natalizumab (tysabri)- adverse effects

A

Major adverse effect: progressive multifocal encephalopathy

169
Q

What are the antibiotics used to treat IBD?

A 
Metronidazole (Flagyl)
Ciprofloxacin
Metronidazole + ciprofloxacin
Rifamixin
Clarithromycin
170
Q

Metronidazole (Flagyl)- indications

A

For treatment of ileocolitis or colitis
Failure to respond to sulfasalazine
For treatment of abscesses, rectovaginal fistulas, proctocolectomy wounds
Low dose maintenance therapy to minimize recurrence of perineal disease

171
Q

Metronidazole (Flagyl)- ADRs

A

GI upset, metallic taste, paresthesias, antabuse-like rxn

172
Q

Ciprofloxacin

A

Effective in resistant disease when used in combination with standard tx

173
Q

Metronidazole + ciprofloxacin

A

Improve and can promote closure of fistulas

Tend to recur once drugs stopped

174
Q

Rifamixin

A

Data from open-label trial found statistically significant response in mild-moderate disease

175
Q

Clarithromycin

A

Response in pts otherwise unresponsive

176
Q

Opiates

A

Provide symptomatic relief of diarrhea
Diphenoxylate/atropine, codeine, tincture of opium, paregoric, loperamide
MOA: inhibits excessive GI motility and GI propulsion

Pharmacology II (23 decks)

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