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226 Cards in this Set

  • Front
  • Back
examples of asthma drugs
Glucocorticoids
BECLOMETHASONE
fluticasone
PREDNISONE
examples of asthma drugs
Mast Cell Stablizers
CROMOLYN SODIUM
examples of asthma drugs
CROMOLYN SODIUM
Mast Cell Stablizers
examples of asthma drugs
Leukotriene Inhibitors
MONTELUKAST (SINGULAIR)
ZILEUTON
Zarkulast
examples of asthma drugs
Selective beta2-Adrenergic Receptor Agonists
ALBUTEROL
EPINEPHRINE
terbuteline
salmeterol
examples of asthma drugs
"Other" Bronchodilators
IPRATROPIUM
THEOPHYLLINE
examples of asthma drugs
Immunoglobulin Antagonist
OMALIZUMAB (XOLAIR)
examples of asthma drugs
Antitussives
CODEINE
dextromethorphan
examples of asthma drugs

Expectorants
GUAIFENESIN
IODINE
water
examples of asthma drugs

Antihistamines
FEXOFENADINE
DIPHENHYDRAMINE
General class of drug
BECLOMETHASONE
Anti-inflammatory Drugs
Glucocorticoids
General class of drug

CROMOLYN SODIUM
Anti-inflammatory Drugs
Mast Cell Stablizers
General class of drug

MONTELUKAST
Anti-inflammatory Drugs
Leukotriene Inhibitors
General class of drug

ZILEUTON
Anti-inflammatory Drugs
Leukotriene Inhibitors
General class of drug

fluticasone
Anti-inflammatory Drugs
Glucocorticoids
General class of drug

PREDNISONE
Anti-inflammatory Drugs
Glucocorticoids
General class of drug

ALBUTEROL
Bronchodilators
Selective beta2-Adrenergic Receptor Agonists
General class of drug

terbuteline
Bronchodilators
Selective beta2-Adrenergic Receptor Agonists
General class of drug

salmeterol
Bronchodilators
Selective beta2-Adrenergic Receptor Agonists
General class of drug

IPRATROPIUM
Bronchodilators
Anticholinergic drugs
General class of drug

THEOPHYLLINE
Bronchodilators
Non-Selective PDE Inhibitor
General class of drug

OMALIZUMAB (XOLAIR)
Immunoglobulin Antagonist
General class of drug

CODEINE
Antitussives
General class of drug

dextromethorphan
Antitussives
General class of drug

GUAIFENESIN
Expectorants
General class of drug

IODINE
Expectorants
General class of drug
FEXOFENADINE
Antihistamines
General class of drug
DIPHENHYDRAMINE
Antihistamines
Broncodilators mechs
-beta 2 agonists increases CAMP
-Theophyline increases CAMP to 5'AMP
-IPRATROPIUM blocks Ach via M3 receptor stimulation leading to decrease in cytosolic Ca
besides smooth muscle relaxation what else do beta 2 agonists do for asthma patients
-stimulation of mucociliary

decreae muscle hypertrophy and hyperplasia

-inhibit inflammatory cells

-increase in NO
What mediates the helpful effects of the beta 2 agonists
cAMP
what is the long acting beta2 agonist? Time?
Salmeterol

12 Hours
Selective β2 adrenergic agonists
Major side effects
tremor
Bronchodilators
what are the anticholinergics used for
usually COPD, not asthma
Theophylline
prototype of wwhat drug class
Methylxanthine
Non-selective PDE inhibitor
Adverse effects may be related to PDE3 inhibition
Theophylline: and all other Methylxanthines
why do you need to monitor blood levels of Theophylline
-Drug and food interactions
-Wide blood level variation (i.e., elderly, smokers)
Theophylline
toxicity effects in order as dose increases
-GI Upset and
-nervousness
-Arrthythmias
-Convulsions
Factors affecting theophylline clearance
clearance increased by: young, cigarrete smoking, pregnancy, OCP

Decreased by :old age, Liver disease, Alcoholism, Fever, Viral, infection, drugs, CHF, obesity
Factors affecting theophylline clearance
specific Drugs
ALL DECREASE CLEARANCE
Cimetidine
Allopurinol
Propranolol
Macrolide antibotics
Cromolyn Sodium
MOA
-affects delayed chloride channels in cell membranes
-inhibits Ca++ influx
Cromolyn Sodium
cellular effects
airway nerves → ↓inhibit cough
↓inflammatory mediators
↓ eosinophil infiltration
Zafirlukast
moa
-Inhibition of leukotrienes
-↓ both early and late inflammatory phases
Zafirlukast
adverse effects
headache
nausea & diarrhea
infection
zileuton
moa
-Inhibition of leukotrienes
-selective 5 - lipoxygenase inhibitor
zileuton
adverse effects
hepatic toxicity
headache
dyspepsia
Omalizumab
moa
antibody blocks only the specific region of IgE that binds to mast cells
Omalizumab
how administered
Not orally active – requires SC administration every 2-4 weeks
Omalizumab
adverse effects
-headache
-viral infection
-thrombocytopenia?
-allergic reactions
No other expectorant is superior
water
Oral mucokinetic agents
-potassium iodide
-guaifenesin (glyceryl guaiacolate)
dornase alpha
class
Expectorants
dornase alpha
moa
recombinant human deoxyribonuclease (rhDNase)
Mechanism of action
dornase decrease sputrum viscosity by cleaving
extracellular DNA into smaller fragments
dornase alpha
Therapeutic use
-cystic fibrosis
-chronic bronchitis
dornase alpha
Adverse effects
-coughing and wheezing
-hemoptysis
-pharyngitis
antibodies to ?????? have not been detected

drug for CF
dornase alpha
Autacoids and Antihistamines
Name the
H1 receptor antagonists
DIPHENHYDRAMINE
CHLORPHENIRAMINE
FEXOFENADINE
Autacoids and Antihistamines
Name the
H2 receptor antagonists
CIMETADINE and others
Autacoids and Antihistamines
Name the
5-HT agonists
BUSPIRONE
sumatriptan
tegaserod
Autacoids and Antihistamines
Name the
5-HT antagonists
clozapine
cyproheptadine
ONDANSETRON
METHYSERGIDE
General class of drug

DIPHENHYDRAMINE
Autacoids and Antihistamines
H1 receptor antagonists
Autacoids and Antihistamines
Name the
Endothelin-1 Antagonists
BOSENTAN
Autacoids and Antihistamines
Name the
Prostaglandins
ALPROSTADIL
CARBOPROST
MISOPROSTAL
DINOPROSTONE
EPOPROSTANOL
latanoprost
General class of drug
CHLORPHENIRAMINE
Autacoids and Antihistamines
H1 receptor antagonists
General class of drug
FEXOFENADINE
Autacoids and Antihistamines
H1 receptor antagonists
General class of drug
CIMETADINE
Autacoids and Antihistamines
H2 receptor antagonists
General class of drug
BUSPIRONE
Autacoids and Antihistamines
5-HT agonists
General class of drug
ONDANSETRON
Autacoids and Antihistamines
5-HT antagonists
General class of drug
METHYSERGIDE
Autacoids and Antihistamines
5-HT antagonists
General class of drug
ALPROSTADIL
Autacoids and Antihistamines
Prostaglandins
General class of drug
CARBOPROST
Autacoids and Antihistamines
Prostaglandins
General class of drug
MISOPROSTAL
Autacoids and Antihistamines
Prostaglandins
General class of drug DINOPROSTONE
Autacoids and Antihistamines
Prostaglandins
General class of drug EPOPROSTANOL
Autacoids and Antihistamines
Prostaglandins
General class of drug
BOSENTAN
Autacoids and Antihistamines
Endothelin-1 Antagonists
Physiologic role
H1 receptors
-Allergy
-inflammation
-Tissue growth, wound healing, keloid and scar formation
-Urticaria
-Cough reflex
Physiologic role
H2 receptors
-Allergy
-inflammation
-Gastric acid secretion
Physiologic role
H3 receptors
↑ presynaptic receptors to ↓ neurotransmitter release
different H receptors are coupled to
-H1 receptors are coupled to inositol triphosphate (IP3) and diacylglycerol (DAC).
-H2 receptors activate G-proteins to increase adenyl cylase activity
-H3 receptors are primarily presynaptic and coupled to G-proteins
Antihistamines
Mechanism of Action
Unrelated to H1-receptor blockade
-Blockade of cholinergic muscarinic receptors (dose-dependent)
-Local anesthesia
-Cardiac effects (membrane stabilizing)
-Alpha-adrenergic receptor blockade promethazine
Antihistamines
Adverse Effects
-CNS
-GI tract
-atropine-like effects
-allergy: usually from topical application
-teratogenesis: piperazines
Antihistamines
drug interaction
with erythromycin and ketoconazole causes torsade de pointe
Antihistamines
acute poisoning
ANTICHOLINERGIC effects (hot as a here ...)
kids go up then down

adults just go down
Antihistamines
acute poisoning Tx
-Generally supportive
-Physostigmine to counter the central anti-cholinergic actions
Antihistamines
some lesser known uses
-Parkinsonism
-petit mal seizures
-local anesthesia
Antagonists of H2-receptors
clinical uses
primarily duodenal ulcer
Eicosanoids
Therapeutic Uses
OB
Vascular disease
CABG
Broncospasm
ED
...
Bosentan
moa
Endothelin-1 Antagonists
ETA and ETB antagonist
Bosentan
Therapeutic use
-pulmonary hypertension
-coronary reperfusion
Drug for
pulmonary hypertension
coronary reperfusion
Bosentan
Bosentan
Adverse effects
-hepatotoxic
-birth defects
Drugs for Migraine Headaches
classes that abort
-5-HT1D/1B agonists
-MISC
5-Hydroxytryptamine (5-HT)
aka
serotonin
serotonin
aka
5-Hydroxytryptamine (5-HT)
5-Hydroxytryptamine (5-HT)
function
5-HT1 receptors:presynaptic effects, vasoconstriction

5-HT2 receptors: vasoconstriction, antiplatelet effects
methysergide
nonselective inhibition of vasoconstrictor and pressor actions of 5-HT. It also is a partial agonist
nonselective inhibition of vasoconstrictor and pressor actions of 5-HT. It also is a partial agonist
methysergide
cyproheptadine
nonselective antagonizism of the effects of 5-HT on smooth muscle. Also blocks H1 and muscarinic receptors
nonselective antagonizism of the effects of 5-HT on smooth muscle. Also blocks H1 and muscarinic receptors
cyproheptadine
Ergot Alkaloids
Pharmacokinetics
-Poorly and irregularly absorbed from the GI tract due to high molecular weight
-Probably metabolized in the liver
Ergot Alkaloids
uses wrt preg
-uterus at term is very sensitive
-long sustained contractions are not suitable for induction of labor
-ergonovine and methylergonovine are used to control post partum hemorrhage
Adverse effects of ergotamine
-GI
-arteriospastic effects
-muscle weakness
-hypersensitivity – localized edema and itching
Triptans
name
Sumatriptan
Short DOA → rebound headaches
Sumatriptan
name the
5-HT1D/1B agonists
and there uses
Buspirone – antidepressant
SSRIs
Sumatriptan – migraine
Ergot alkaloids - migraine and post partum bleeding
Tegaserod –IBS
name the 5-HT Drugs
Antagonists
and there uses
-Clozapine – antipsychotic
-Cyproheptadine – also H1 antagonist
-Methysergide – migraine
-Ondansetron – antiemetic
-ketanserin - HTN
Migraine
DOC for acute attacks
ergotamine
ergotamine is effective in terminating migranes because
-Vasoconstriction (partial agonist activity)
-Presynaptic effects ↓ release of inflammatory and pain peptides
-prazole
Proton pump inhibitors
PPI
name them
omeprazole, lansoprazole, rabeprazole, esomeprazole and pantoprazole
name the
H2-receptor antagonists
cimetidine,
.... -tidine
cimetidine,
.... -tidine
H2-receptor antagonists
name the M1-muscarinic receptor antagonists
-antheline
and
-ZEPINE
name the
Laxatives:
castor oil,
emodin alkaloids phenolphthalein,
bisacodyl
Bulk forming laxatives
name the Stool softeners
docusate,
glycerin suppositories,
mineral oil
name the Opioids Antidiarrheals
diphenoxylate,
loperamide,
difenoxin,
paregoric
name the Absorbants Antidiarrheals
bismuth subsalicylate,
kaolin,
pectin
name the Emetics:
ipecac, apomorphine
name the Antiemetics:
scopolamine, dimenhydrinate, meclizine, cyclizine, dronabinol, ondansetron, granisetron
name the Gastrointestinal reflux disease drugs (not PPI H2 blocker or ntacid)
metoclopramide, cisapride
name the Inflammatory Bowel Disease drugs
5-aminosalicylic preparations: sulfasalazine, olsalazine, mesalamine (several formulations).

Corticosteroids: hydrocortisone, prednisone.
name the Anticholelithics
ursodiol, chenodiol, monoctanoin
name the IBS drugs
tegaserod,
alosetron
Gastric acid secretion by the parietal cell is under the control of 3 agonists:
histamine
Ach
gastrin
PPI MOA
oxidizes - SH groups in the pump after it is converted to the sulfenamide derivative. It inhibits acid secretion elicited by every stimulus, irreversible.
Drug of choice for Zollinger-Ellison syndrome
Omeprazole
Most effective drugs for treating gastroesophageal reflux disease
PPI
-tidine
side effects
reduce male sexual function
gynecomastia
menstrual disorders
Misoprostol
moa
Agents that Increase Resistance of Mucosa to Acid-Peptic Digestion
-prostaglandin E1 analog
Sucralfate
moa
Agents that Increase Resistance of Mucosa to Acid-Peptic
-residual compound becomes negative and polymerizes to form a viscous paste
Colloidal Bismuth subsalicylate
moa
bismuth subsalicylate reacts with hydrochloric acid to form bismuth oxychloride and salicylic acid
Triple-drug therapy treatment recommended for H. pylori infection
drugs
1.Bismuth subsalicylate (Pepto-Bismol)
2. Metronidazole (Flagyl)
3. Tetracycline or amoxicillin (Amoxil, Wymox)
Helidac -
three tablets (Triple-drug therapy treatment recommended for H. pylori )
Systemic Antacids
Sodium bicarbonate, sodium citrate
Systemic Antacids
adverse effects
-alkalosis
-urinary tract infection by altering urinary pH.
Calcium Carbonate
Adverse effects
hypercalcemia
Magnesium hydroxide
Adverse effects
diarrhea
Aluminum hydroxide
uses
antacid
Aluminum hydroxide
Adverse effects
constipation
Milk-Alkali Syndrome
Systemic antacids and large amounts of milk produce headache, weakness, nausea, and vomiting. Hypercalcemia, mild alkalosis stone formation in kidney, calcification-renal failure.
Bisacodyl
uses
laxatives
Irritant or stimulant laxatives
Emodin
Danthron
Cascara sagrada
Senna
Aloe
Rhubarb
Objectionable taste; strong cathartic effect; metabolized like other fatty acids.
Castor Oil
Active component is ricinoleic acid an anionic surfactant. It is present as a triglyceride that is hydrolyzed by pancreatic lipase to yield ricinoleic acid. Action in small bowel action within 2 hours.
Castor Oil
laxative that When given orally active after deacetylation by bacteria.
Bisacodyl
Isosmotic solution of polyethylene glycol, used as a colonic lavage solution in preparation for radiologic and endoscopic procedures.
Polyethylene glycol
Polyethylene glycol
uses
used as a colonic lavage solution in preparation for radiologic and endoscopic procedures.
Absorbs liquid in intestines and swells to form soft bulky stool. Bulky mass stimulates intestinal muscles speeding stool transit through colon. Need fluid intake to work.
Polycarbophil
Side Effects of Laxatives
1.Cathartic colon syndrome
2. Addiction
3. hypokalemia
4. malabsorbtion
5. liver probs
Diarrhea Tx
1.replace fluid and electrolytes
2.reduce water in stools and increase absorption
3.drugs
liquid and solid preparation, effective against "traveler's diarrhea" - absorbs enterotoxins from E. coli. Antimicrobial action against E. coli inhibits PG production and cAMP levels
Pepto-Bismol, bismuth subsalicylate
kaolin/pectin
moa
Antidiarrheal effect of opiates related to effects on smooth muscle and mucosa increasing electrolyte transport.
Opiates anti diarrheal
moa
Nerve plexuses within bowel wall inhibiting release of acetylcholine. Enkephalin receptors found in CNS and gastrointestinal tract - µ receptors
major metabolite of diphenoxylate, 5 times more potent, action on CNS side effect
Difenoxin
(Lomotil combined with atropine) analog of meperidine (Demerol) similar actions to morphine. No analgesic activity in therapeutic range.
Diphenoxylate
opiate analog, effects on gastrointestinal motility similar to those of morphine. Acts on opiate receptors (naloxone blocks)
Loperamide
Loperamide wrt adiction
-no analgesic activity
-no CNS effect
-used chronically (1 year) no tolerance or dependence; only minor side effects
Ipecac
moa
chemoreceptor trigger zone (CTZ) in the fourth ventricle of the brain,
Ipecac timing
it has a delayed onset of action.
Vomiting in 85% of patients within 20 min.
Apomorphine
uses
Emetics
Apomorphine
moa
It also acts on the CTZ but since it is given by injection
Apomorphine
timing
It also acts on the CTZ but since it is given by injection (subcutaneously) it has an onset of action of a few minutes
Apomorphine
other use
Dopamine analog, also used to treat Parkinson's disease.
Scopolamine:
moa
An anticholinergic agent
are usually employed to treat postoperative nausea and vomiting, as well as that induced by radiation therapy. Oral also rectal and IV.
Phenothiazines e.g., chlorpromazine (Thorazine)
Treating anorexia associated with weight loss in AIDS patients. Acts on vomiting center, mechanism unknown.
Cannabinoids
Ondansetron (ZOFRAN), granisetron (KYTRIL).
moa
antiemitic
5-HT­3 antagonists
Given orally or IV before cancer chemotherapy, well tolerated. Metabolized in liver. Selectively blocks 5-HT3 receptors in the periphery and the brain (chemoreceptor trigger zone).
5-HT­3 antagonists. Ondansetron (ZOFRAN), granisetron (KYTRIL).
Metoclopramide
moa
GERD
Increase tone of esophageal sphincter
Metoclopramide
adverse effects
-Increase sensitivity of intestinal smooth muscle to acetylcholine;
-can cause diarrhea.
Cisapride
moa
GERD
Increases contractility of intestinal musculature, gastric and lower esophageal sphincter tone and esophageal motility
themes in therapy of Chronic Inflammatory Bowel Disease (ulcerative colitis, Chron’s disease).
Treatment involves use of salicylate derivatives, corticosteroids and immunosuppressive agents.
Inhibit prostaglandin and leukotriene formation. High doses cause upper gastrointestinal tract irritation. Several preparations available.
Mesalamine
Salicylates
Mesalamine preparatins (Asacol
Pentasa Rowasa)
Mesalamine aka
5-ASA
Mesalamine
uses of
XIII.Chronic Inflammatory Bowel Disease (ulcerative colitis, Chron’s disease).
Treatment involves use of salicylate derivatives,
Mesalamine
adverse effects
watery diarrhea,
some nephrotoxicity
and pancreatitis.
After oral administration about one-third is absorbed from the small intestine. The remaining two-thirds pass to the colon where the azo bond in the compound is split by intestinal bacteria into 5-ASA and sulfapyridine.
Sulfasalazine
Sulfasalazine
adverse effects
Most of the sulfapyridine is absorbed and about one-third of the 5-ASA is absorbed, the remainder ends up in feces. Sulfapyridine can cause significant toxicity:
-bone marrow suppression, -liver failure,
-impair male fertility.
links two 5-ASA molecules via an azo bond that is broken down by bacteria in the colon to release 5-ASA
Olsalazine
Olsalazine absorbtion
After oral administration only 2% of olsalazine enters the circulation, the remainder reaches the colon.
Infliximab
moa
Chimeric IgG monoclonal antibody for the treatment of Crohn’s disease. Neutralizes the biological activity of TNF-.
Infliximab
adverse reactions
- infusion reactions
-infections.
Drugs for dissolution of gallstones (anticholelithics).
Chenodiol, chenodeoxycholic acid (Chenix) and ursodiol, ursodeoxycholic acid the 7-epimer of chenodiol (Actigall) are effective at dissolving stones in some patients. Oral.
Chenodiol
moa
inhibits 3-hydroxy-3-methylglutaryl-CoA reductase, rate limiting enzyme in the synthesis of cholesterol in the liver
Chenodiol
adverse effects
Requires long term treatment (2 years). Adverse side effect is diarrhea in 30% of patients.
Ursodiol
moa
inhibits intestinal absorption of dietary and biliary cholesterol. Also promotes mobilization of cholesterol from gallstones.
Ursodiol
adverse effects
Less diarrhea than chenodiol.
infused (24 hours) into common bile duct to dissolve retained bile duct stones. The remaining 20% is other fatty acid esters and glycerol
Monoctanoin
Monoctanoin
adverse effects
. Fatigue,
abdominal pain,
nausea,
vomiting,
diarrhea
pruritus.
is for the short-term treatment of women who have IBS with constipation
Tegaserod maleate
Tegaserod maleate
uses
women who have IBS with constipation
Alosetron
uses
Irritable bowel syndrome (IBS) with diarrhea
drug for Irritable bowel syndrome (IBS) with diarrhea
Alosetron
Name the Nonsteroidal Anti-inflammatory Drugs
nonselective
Aspirin
Ibuprofin
Naproxen
Ketolac
Name the COX-2
Celecoxib
Name the COX-3
Acetomenophin
Name the DMARDS
Methotrexate
Hydroxychloroquine
Etanercept
Infliximab
sulfasalazine
Name the drugs to prevent gout attacks
probenacid
sulinpyrazole
allopuranol
Name the to Tx gout attacks
colchicine
NSAIDs (indomethicin)
NSAIDs
Other Adverse Effects
dyspepsia
Analgesic or urate nephropathy
Inhibition of renal PG’s
Asthma
Skin rashTinnitus
Headache, drowsiness, dizziness,
fatigue
Reye’s syndrome
Aspirin:
Treatment of Overdose
Induce vomiting/gavage
NaHCO3 IV
Counteract metabolic acidosis
Acetaminophen
interactions
acetaminophen/warfarin
acetaminophen/alcohol
acetaminophen/alcohol
effects
intermediate metabolite NAPQI bulds up bc increased P450 action and decreased amount of glutathione
Single most effective DMARD
Methotrexate
Methotrexate
moa
↓ folate reductase
↓ lymphocyte proliferation
↓ cytokines and rheumatoid factor production
↓ leucocyte chemotaxis
↓ production of free radicals and other cytotoxins
Methotrexate
adverse effects
Hepatoxicity, bone marrow suppression, teratogenic
Methotrexate
class of drug
DMARDS
-Antineoplastic and immunomodulatory
etanercept
moa
DMARD
Immunomodulators
– human TNF receptor + Fc fragments of IgG
Bind to and ↓ TNF
infliximab
moa
DMARD
Immunomodulators
monoclonal Ab for TNF

Bind to and ↓ TNF
adalimumab
moa
DMARD
Immunomodulators
monoclonal Ab for TNF

Bind to and ↓ TNF
Least toxic DMARD but slow onset > 6 mo
Hydroxychloroquine
↓ lymphocytes, PMN’s, superoxide radicals
G6PD deficiency → hemolytic anemia
Retinal damage in elderly
Hydroxychloroquine
DMARDS
?MOA
Sulfasalazine
MOA ???
Nausea, rash,
G6PD deficiency → hemolytic anemia
Leukopenia, hepatitis
Sulfasalazine
Gold Salts
adverse effects
Hematologic
Dermatologic
GI
renal
Reduce uric acid synthesis
Allopurinol
-Purine (uric acid) analog inhibits xanthine oxidase
Allopurinol
adverse effects
Nausea,
vomiting,
hypersensitivity
hepatitis,
skin rash
inhibit reabsorption of uric acid by renal tubules
probenecid,and sulfinpyrazone
probenecid
moa
inhibit reabsorption of uric acid by renal tubules
sulfinpyrazone
moa
inhibit reabsorption of uric acid by renal tubules
colchicine
moa
decrease tubulin synthesis → decrease leucocyte mobility
decrease tubulin synthesis → decrease leucocyte mobility
colchicine
colchicine
adverse effects
nausea,
vomiting,
diarrhea,
cramps
NSAID for Gout
Indomethacin
Indomethacin
uses
NSAID for Gout