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681 Cards in this Set

  • Front
  • Back
Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
Half-life (t1/2)
Relates the amount of drug in the body to the plasma concentration
Volume of Distribution (VD)
Plasma concentration of a drug at a given time
Cp
The ratio of the rate of elimination of a drug to its plasma concentration
CL Clearance
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
The fraction of administered dose of a drug that reaches systemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady State
This step of metabolism makes a drug more hydrophilic and hence augments elimination
Phase I
Different steps of Phase I
Oxidation
Reduction
Hydrolysis
Inducers of Cytochrome P450 (4)
Barbituates
Phenytoin
Carbamazepine
Rifampin
Inhibitors of CYP450 (5)
Cimetidine
Ketoconazole
Erythromycin
Isoniazid
Grapefruit
Products of Phase II Conjugation (3)
Glucuronate
Acetic Acid
Glutathione Sulfate
Type of kinetics when a constant PERCENTAGE of substrate is metabolized per unit time
First Order Kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration
Zero Order Kinetics
Cp x (VD/F)

Target plasma concentration times (Volume Distribution divided by bioavailability)
Loading Dose
Cp x (CL/F)

Plasma Concentration x (Clearance divided by Bioavailability)
Maintenance Dose
Strength of interaction between drug and its receptor
Affinity
Selectivity of a drug for its receptor
Specificity
Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
Potency
Maximum response achievable from a drug
Efficacy
Ability of a drug to produce 100% of the maximum response regardless of the potency
Full Agonist
Ability to produce less than 100% of the response
Partial Agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive Antagonist
Class of drugs with the ability to decrease the maximal response to an agonist
Noncompetitive Antagonist
A hormone whose MOA utilizes intracellular receptors
Thyroid and Steroid Hormones
A hormone whose MOA utilizes transmembrane receptors
Insulin
Class of drugs whose MOA utilizes ligand gated ion channels
Benzodiazepines and Calcium Channel Blockers
Median Effective dose required for an effect in 50% of population
ED50
Median toxic dose required for a toxic effect in 50% of population
TD50
Dose which is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic Index
Term for high margin of safety
High Therapeutic Index
Term for a narrow margin of safety
Low Therapeutic Index
Antidote used for lead poisoning
Dimercaprol, EDTA
Antidote used for cyanide poisoning
Nitrites
Antidote used for anticholinergic poisoning
Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning
Atropine
Pralidoxime (2-PAM)
**
Antidote used for iron salt toxicity
Deferoxamine
Antidote used for Acetaminophen (APAP) Toxicity
N-acetylcysteine (NAC)
Mucomyst
*
Antidote for arsenic, mercury, lead, and gold poisoning
Dimercaprol
Antidote used in poisonings - Cooper (Wilson's), lead, mercury, and arsenic
Penicillamine
Antidote used for heparin overdose
Protamine
**
Antidote used for Warfarin toxicity
Vit K
Fresh Frozen Plasma (FFP)
*
Antidote for t-PA, streptokinase
Aminocaproic Acid
**
Antidote used for methanol and ethylene glycol
Ethanol or
Fomepizole
Antidote used for opioid toxicity
Naloxone (IV)
Naltrexone (PO)
*
Antidote used for Benzodiazepine Toxicity
Flumazenil
*
Antidote used for Tricyclic Antidepressants (TCA)
Sodium Bicarbonate
Antidote used for Carbon Monoxide Poisoning
100% O2 and hyperbaric O2
Antidote used for Digitalis Toxicity
Digibind

also d/c digoxin, normalize K+, lidocaine is arrhythmic
Antidote used for B-agonist Toxicity (metaproterenol)
Esmolol
Antidote for methotrexate toxicity
Leucovorin
Antidote for B-blockers and hypoglycemia
Glucagon
Antidote useful for some drug induced Torsade de Pointes
Magnesium Sulfate
Antidote for Hyperkalemia
Sodium Polystyrene Sulfonate (Kayexalate)
Antidote for salicylate intoxication
Alkalinize Urine
Dialysis
Constant proportion of cell population killed rather than a constant number
Log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse Therapy
Toxic effect of anticancer drug can be lessened by rescue agents
Rescue Therapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Allopurinol
Pyrimidine analog that causes "Thymine-less Death" given with leucovorin rescue
5-fluoracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
Side effect of Mitomycin
SEVERE myelosuppression
MOA of Cisplatin
Alkylating Agent
Common Toxicities of Cisplatin
Nephro and ototoxicity
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6-MP
Allopurinol
**
May protect against doxorubicin toxicity by scavenging free radicals
Dexrazoxane
*
Blows DNA (breaks DNA stands), limiting SE is pulmonary fibrosis
Bleomycin
*
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
Testicular Cancer
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +
Bleomycin +
Vinblastine +
Dacarbazine
Regimen used for nonHidgkin's Lymphoma
CHOP
(Cyclophosphamide
Doxorubicin
Vincristine
Prednisone)
+Rituximad
Regimen used for breast cancer
CMF
(Cyclophosphamide
Methotrexate
Fluorouracil)
+Tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation
Mechlorethamine
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
Prevention of cyclophosphamide induced Hemorrhagic Cystitis
Hydration and Mercaptoethanesulfonate (MENSA)
Microtubule inhibitor that causes peripheral neuropathy, foot drop (ataxia), and pins&needles sensation
Vincristine
Interacts with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and -cells remain frozen in metaphase-
Paclitaxel (taxol)
**
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Cisplatin
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Carboplatin
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
L-asparaginase
Used for HCL (Hairy Cell Leukemia); it stimulates NK cells
INF-a
Anti-androgen used for prostate cancer
Flutamide (Eulexin)
Anti-estrogen used for ER Breast Cancer
Tamoxifen
**
Aromatase inhibitor used in BC
Letrozole
Anastrozole
Newer Estrogen Receptor antagonist used in advanced BC
Toremifene (Fareston)
Some cell cycle specific anti-cancer drugs (6)
Bleomycin
Vinca Alkaloids
Antimetabolites (4) - 5-FU, 6-MP, Methotrexate, Etoposide
Some cell cycle non-specific drugs (6)
Alkylating Agents (Mechlorethamine, Cyclophosphamide)
Antibiotics (Doxorubicin, Daunorubicin)
Cisplatin
Nitrosourea
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 antagonists (Serotonin Receptor subtype)
Odansetron
Granisetron
*
Nitrosoureas with high lipophilicity, used for -brain tumors-
Carmustine (BCNU)
Lomustine (CCNU)
Produces disulfiram-like reaction with ethanol
Procarbazine
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma, and other GH producing pituitary tumors
Octeotide
Somatotropin (GH) analog used in GH deficiency (dwarfism)
Somatrem
GHRH analog used as diagnostic agent
Sermorelin
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
Ganirelix
Dopamine (DA) agonist (used for Parkinson's), used also for hyperprolactinemia
Bromocriptine
*
Hormone inhibiting prolactin release
Dopamine
*
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Cosyntropic
**
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
SE of OCs

OCs?
Increased thromboemoblic events
**
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
L-thyroxine (T4)
T3 compound less widely used
Cytomel
Anti-thyroid drugs (4)
Thioamides
Iodides
Radioactive Iodine
Ipodate
Thomaide agents used in hyperthyroidism (2)
Methimazole
Propylthiouracil (PTU)
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
Propylthiouracil (PTU)
*
PTU (Propylthiouracil) MOA?
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
Can be effective for -short term therapy- of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide Salts
Dose may need to be increased during pregnancy or with OCs due to increased TBG in plasma
Thyroxine
**
-Permanently cures thyrotoxicosis-, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Radioactive Iodine
-Radio contrast media- that inhibits the conversion of T4 to T3
Ipodate
Block cardiac adverse effects of thryotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
B-blockers (propranolol)
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
Iron deiodinates thyroxine
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
Estrogens increase maternal TBG (thyroxine binding globulin)
3 zones of adrenal cortex and their products
Glomerulosa (Mineralocorticoids)
Fasiculata (Glucocorticoids)
Reticularis (Adrenal Androgens)
Pneumonic for 3 zones of Adrenal Cortex
GFR

salt sugar sex
Used for Addison's Diease, Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
Glucocorticoids
Short acting Glucocorticoids (2)
Cortisone
Hydrocortisone (equivalent to cortisol)
Intermediate acting GCs (4)
Prednisone
Methylprednisolone
Prednisolone
Triamcinolone
Long acting GCs (2)
Betamethasone
Dexamethasone
Mineralocorticoids (2)
Fludrocortisone
Deoxycorticosterone
Some side effects of Corticosteroids (11 lol)
Osteopenia, impaired healing, increased infection risk, increased appetite, HTN, edema, euphoria, psychosis, stria, thinning of skin
Period of time of therapy after which GC therapy will need to be tapered
5 to 7 days
Used for Cushing's Syndrome (increased corticosteroid)

~diagnosis
Dexamethasone Suppression Test
Inhibits conversion of cholesterol to Pregnenolone therefore inhibiting corticosteroid synthesis
Aminoglutethimide
Antifungal agent used for inhibition of all gonadal and adrenal steroids
Ketoconazole
Antiprogestin used as potent antagonist of GC receptor
Mifepristone
Diuretic used to antagonize aldosterone receptors
Spironolactone
*
Common SE of spironolactone
Gynecomastia and Hyperkalemia
**
Slightly increased risk of BC, Endometrial Cancer, Heart Dz, has beneficial effects on bone loss
Estrogen
Antiestrogen drugs used for fertility and breast cancer respectfully
Clomiphene and Tamoxifen
Common SE of Tamoxifen and Raloxifene
Hot Flashes
Selective Estrogen Receptor Modulator (SERM) used for -prevention of osteoporosis- and prophylaxis in women with increased risk factors for breast cancer
Raloxifene
**
Non-steroidal estrogen agonist causes -Clear Cell Adenocarcinoma of the Vagina- in daughters of women who used it during pregnancy
Diethylstibestrol (DES)
Estrogen most commonly used in OCs
Ethinyl Estradoil and mestranol
Anti-progresterone used as abortifacient
Mifepristone (RU-486)
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 dats are sugar pills or iron prep)
Combination OCs
Oral Contraceptive available in transdermal patch
Ortho-Evra
Converted to DHT (more active form) by 5a-reductase
Testosterone
5a-reductase inhibitor used for BPH and male pattern baldness
Finasteride (Proscar and Propecia respectively)
Anabolic steroid that has potential for abuse (3)
Nandrolone
Oxymetholone
Oxandrolone
Anti-androgen used for hirsutism in females
Cyproterone Acetate
Drug is used with testosterone for male fertility
Leuprolide
**
What do alpha cells in the pancreas produce?
Glucagon
What do beta cells in the pancreas produce?
Insulin
Where are beta cells found in the pancreas?
Islet of Langerhans
What do delta cells in the pancreas produce?
Somatostatin
Product of proinsulin cleavage used to assess insulin abuse
C-peptide
Exogenous Insulin contains ____ C-peptide
little
*
Endogenous Insulin contains ____ C-peptide
normal
Very rapidly acting insulin, having fastest onset and shortest DoA
Lispro (Humalog)
Aspart
Glulisine
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
Regular (Humulin R)
Long acting insulin
Ultralente (Humulin U)
*
Ultra long acting insulin, has over a day duration of action
Glargine (Lantus)
Detemir
Major SE of Insulin
Hypoglycemia
Important in synthesis of glucose to glycogen in the liver
GLUT2
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase action
GLUT4
Examples of a-glucosidase inhibitors (AGI)
Acarbose
Miglitol
MOA of AGI's
Act of intestine, delay digestion and absorption of glucose formed from digestion of starch and disaccharides
SE of AGI's
Flatulence (don't use Beano to treat), diarrhea, abdominal cramps
AGI associated with elevation of LFTs
Acarbose
Amino Acid derivative, active as an insulin secretagogue
Nateglinide
*
MOA of Nateglinide
Insulin secretagogue, closes ATP-sensitive K+ channel
Biguanide
Metformin
Drugs available in combination with Metformin (3)
Glyburide
Glipizide
Rosiglitazone
MOA of Metformin
decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
Vascular effects of Metformin
Decreased micro and macro vascular disease
Most important potential SE of Metformin
Lactic Acidosis
Incidence of hypoglycemia with metformin
none
Meglitinide class of drugs
Repaglinide
MOA of Repaglinide
Insulin release from pancreas; faster and shorter acting than sulfonylurea
First generation Sulfonylurea (3)
Chlopropamide
Tolbutamide
Tolazamide
etc
2nd generation Sulfonylurea (3)
Glyburide
Glipizide
Glimepiride
etc
MOA of both generations of Sulfonylureas
Insulin release from pancreas by modifying K+ channels
Common SE of sulfonylureas, repaglinide, and nateglinide
hypoglycemia
Sulfonylurea NOT recommended for elderly because of very long half life
Chlorpropamide
thiazolidinediones (3)
Pioglitazone
Rosiglitazone
Troglitazone (withdrawn from market)
Reason Troglitazone was withdrawn from market
Hepatic Toxicity
MOA of thiazolidinediones
Stimulate PPAR-gamma receptor to regulate CHO and Lipid Metabolism
SE of thiazolidinediones
Edema
Mild Anemia
Interaction with CYP450 3A4 metabolized drugs
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycema, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Glucagon
Available bisphosphonates (6) used in bone homeostasis
Alendronate
Etidronate
Risedronate
Pamidronate
Tiludronate
Zoledronic Acid
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
Names of 3 Bisphosphonates available IV
Pamidronate
Zoledronate
Ibandronate
Uses of Bisphosphonates (4)
Osteoporosis
Paget's Disease
Osteolytic Bone Lesions
Hypercalcemia from malignancy
Major SE of bisphosphonates
Chemical esophagitis
Bisphosphonate that -cannot be used on continuous basis- because it caused osteomalacia
Etidronate
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT)
Increase bone density, also being tested for Breast Cancer prophylaxis
Raloxifene (SERM)
**
Used intranasally and decreases bone resorption
Calcitonin (salmon prep)
*
Used especially in postmenopausal women, dosage should be 1500mg (1.5g)
Calcium
Vitamin given with calcium to ensure proper absorption
Vitamin D
Disease caused by excess ergot alkaloids
St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
Drug that causes contraction of the uterus
Oxytocin
*
Distribution of histamine receptors (H1, H2, H3)
H1 - Smooth muscle
H2 - Stomach, Heart, Mast Cells
H3 - Nerve Ending, CNS
Prototype antagonist of H1 and H2 receptors (separate answers)
H1 - Diphenhydramine
H2 - Cimetidine
1st generation anti-histamine that is highly sedating
Diphenhydramine
1st generation antihistamine that is least sedating
Chlorpheniramine
Cyclizine
2nd generation antihistamines (3)
Fexofenadine
Loratadine
Cetirizine
Generation of antihistamine that has most CNS effects
First Generation due to being more lipid-soluble
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and is not addictive
Hydroxyzine (Atarax)
H1 antagonist used in motion sickness (2..)
Dimenhydrinate
Meclizine
other 1st generations
Most common SE of 1st generation antihistamines
Sedation
Lethal arrhythmias resulting from concurrent therapy with azole fungals (CYP3A4 metabolized) and these antihistamines which inhibit CYP3A4 (2)
Terfenadine
Astemizole

both already removed from market
H2 blocker that causes the most interference with other drugs
Cimetidine
*
Clinical use for H2 blockers (3)
Acid Reflux
Duodenal Ulcer
Peptic Ulcer
Receptors for Serotonin (5HT-1) are located (+MoA)
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
5HT-1d agonist used for migraine headaches (3)
Sumatriptan
Naratriptan
Rizatriptan
**
Triptan available in parenteral and nasal formulations
Sumatriptan
H1 blocker that is also a serotonin antagonist
Cyproheptadine
Agents for reduction of postpartum bleeding (3)
Oxytocin
Ergonovine
Ergotamine
**
Agents used in treatment of carcinoid tumor (3)
Ketaserin
Cyproheptadine
Phenoxybenzamine
**
5HT-3 antagonist used in chemotherapeutic induced emesis (4)
Ondansetron
Granisetron
Dolasetron
Alosetron
***
5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
DOC to treat chemo-induced nausea and vomiting
Odansetron
**
Drug used in ergot alkaloid overdose, ischemia and gangrene
Nitroprusside
Reason ergot alkaloids and contraindicated in pregnancy
Uterine Contractions
SE of ergot alkaloids
Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug
LSD
Dopamine agonist used in hyperprolactinemia
Bromocriptine
*
Peptide causing increased capillary permeability and edema
Bradykinin and Histamine
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
Bradykinin
*
Drug causing depletion of Substance P (vasodilator)
Capsaicin
*
Prostaglandins that cause abortions (3)
PGE1
PGE2
PGF2alpha
Difference between COX 1 and COX 2
COX1 is found throughout the body and COX2 is only found in inflammatory tissue
Drug that selectively inhibits COX2 (2)
Celecoxib
Rofecoxib
Inhibitor of Lipoxygenase
Zileuton
*
Major SE of Zileuton
Liver Toxicity
Inhibitor of Leukotrienes (LTD4) receptors and used in asthma (2)
Zafirlukast
Montelukast
Used in pediatrics to maintain patency of Ductus Arteriosis
PGE1
Approved for use in severe pulmonary HTN
PGI2 (Epoprostenol)
Prostaglandin used in the treatment of impotence
Alprostadil
*
Irreversible, nonselective COX inhibitor
Aspirin
Class of drugs that reversibly inhibit COX
NSAIDS
Primary endogenous substrate for Nitric Oxidase Synthase
Arginine
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
*
Long acting Beta-2 agonist used in asthma
Salmeterol
Muscarinic antagonist used in asthma
Ipratropium
*
MOA of Cromolyn
Mast Cell stabilizer
*
Methylxanthine derivative used as a remedy for intermittent claudication
Pentoxifylline
MOA of corticosteroids
inhibition of phospholipase A2
SE of long term (>5days) corticosteroid therapy and remedy
Adrenal Suppression

Weaning slowly
*
MOA of Quinolones
Inhibit DNA Gyrase
**
MOA of penicillin
Block cell wall synthesis by inhibiting peptidogylcan cross-linkage
Drug use for MRSA
Vancomycin
*
Vancomycin MOA
Blocks cell wall synthesis by sequestration
Genetic basis of low level resistance found with vancomycin
point mutation
Meningitis prophylaxis for persons in contact with patients
Ciprofloxacin or Rifampin (for children less than 4 years old)
Technique to treat perianal itchning and drug used to treat it
Scotch Tape Technique
Mebendazole
Two toxicities of aminoglycosides
Nephrotoxicity
Ototoxicity
DOC for Legionnaire's Diease
Moxifloxacin
MOA Sulfonamides
Inhibit dihydropteroate synthase
*
Penicillins active against penicillinase secreting bacteria (3)
Methicillin
Nafcillin
Dicloxacillin
Cheap wide spectrum antibiotic, DOC for otitis media
Amoxicillin
***
Class of antibiotics that have 10% cross sensitivity with penicillins
Cephalosporins
PCN active against pseudomonas (4)
Ceftazidime
Imipenem
Piperacillin
Ticarcillin
Antibiotic causing Red-man syndrome, and prevention
Vancomycin

infusion at a slow rate and antihistamines
Drug causes teeth discoloration
Tetracycline
MOA of Tetracycline
Decreases protein synthesis by inhibiting 30S ribosome
Drug that causes Grey Baby Syndrome and Aplastic Anemia
Choramphenicol
Drug notorious for causing pseudomembranous colitis
Clindamycin
DOC for tx of mild Pseudomembranous Colitis
Metronidazole
**
Treatment of severe/relapsing pseudomembranous colitis
ORAL Vancomycin
Anemia caused by trimethoprim
Megaloblastic Anemia
*
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
DOC for Giardia
Metronidazole
*
DOC for Bacterial Vaginosis
Metronidazole
*
DOC for Trichomonas
Metronidazole
*
Treatment for TB? (+ how to remember)
Rifampin
Isonaizid
Pyrazinamide
Ethambutol

RIPE
Metronidazole SE if given with alcohol
Disulfram-like reaction
Common SE of Rifampin
Red urine discoloration
*
MOA of nystatin
bind ergosterol in fungal cell membrane
Neurotoxicity with isonaizid (INH) prevented by
Administration of Vitamin B6 (pyridoxine)
Toxicity of amphotericin
Nephrotoxicity
SE seen only in men with administration of ketoconazole
Gynecomastia
topical DOC in impetigo
Topical mupirocin (Bactroban)
DOC for Influenza A
Oseltamivir
*
DOC for RSV
Ribavirin
DOC for CMV retinitis
Ganciclovir
SE for Ganciclovir
Neutro/Leuko/Thrombocyto - penia
Anti-viral agents associated with Steven Johnson Syndrome
Nevirapine
Amprenavir
HIV antivirals class known to have severe drug interactions by causing inhibition of metabolism
Protease Inhibitors
*
Antivirals that are teratogens (3)
Delavirdine
Efavirenz
Ribavirin

(DERrrrratorgens)
Antivirals associated with neutropenia (4)
Ganciclovir
Zidovudine
Saquinavir
Interferon
HIV med used to prevent perinatal transmission
Nevirapine
Drug used for African Sleeping Sickness
Suramin
Drug used in Chagas Disease
Nifurtimox
Cephalosporins able to cross BBB (3)
Ceftazidime
Ceftriaxone
Cefotaxime
Oral 3rd generation Cephalosporins NOT able to cross BBB
Cefixime
Drug used for N Gonorrhea in females
Ceftriaxone
*
Cephalosporin causes kernicterus in neonates (2)
Ceftriaxone
Cefuroxime
SE of INH
Peripheral Neuritis and Hepatitis
Aminoglycoside that is least ototoxic
Streptomycin
Drug used in exoerythrocytic cycle of malaria
Primaquine
Oral antibiotic of choice for moderate inflammatory acne
Minocycline
DOC for Leprosy (3)
COMBINATION OF:
Dapsone
Rifampin
Clofazimine
DOC for Herpes and its MOA
Acyclovir

phosphorylation, incorperation into viral DNA, and chain termination
*
Anti-bacterials that cause hemolysis in G6PD deficient patients
Sulfonamides
*
MOA of Erythromycin
Inhibition of protein synthesis at the 50S subunit of ribosome
Antibiotic frequently used for Chronic UTI prophylaxis
Sulfamethoxazole/Trimethoprim (TMP/SMX)
Lactams that can be used in PCN allergic patients
Aztreonam
Carbapenems
SE of Imipenem
Seizures
Antiviral with a dose limiting toxicity of Pancreatitis
Didanosine
Common side effect of hypnotic agents
sedation
Occurs when sedative hypnotics are used chronically or at high doses
tolerance
The most common type of drug interaction of sedative products with other depressant medications
Additive CNS depression
Benzodiazepines used to promote sleep (3)
Temazpan
Trizolam
Flurazepam
Benzodiazepam used for anxiety
alprazolam
non-Benzodiazepine used as an anxiolytic
Buspirone
Non-Benzodiazepine used for sleep
Zolpidem
Major effect of benzodiazepines on sleep at high doses
REM is decreased
*
Neurologic SE of benzos
Anterograde amnesia
Reason benzos are used cautiously in pregnancy
Ability to cross placenta
*
Main route of metabolism for benzos
Hepatic
Benzodiazepines that undergo extrahepatic metabolism (useful in older or hepatically impaired patients) (3)
Lorazepam
Oxazepam
Temazepam
MOA for Benzodiazepines
Increase the frequency of GABA mediated chloride channel opening
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
Flumazenil
*
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
Diazepam
Benzodiazepine that has efficacy against absence seizures and in anxiety states such as agoraphobia
Clonazepam
Benzodiazepines most effect in the treatment of panic disorder (2)
Alprazolam
Clonazepam
Benzodiazepine that is used for anesthesia
Midazolam
DOC for status epilepticus
Diazepam
Longer acting benzodiazepine used in the management of withdrawal states of alcohol and other drugs (comb of 2)
Chlordiazepoxide
Diazepam
Agents having active metabolites, long half lives, and high incidence of adverse effects (4)
Diazepam
Flurazepam
Chlordiazepoxide
Clorazepate
Barbituates may precipitate this hematologic condition
Acute intermittent porphyria
Barbituates decrease the effectiveness of many other drugs via the pharmacokinetics property
Liver enzyme INDUCTION
Barbiturates MOA
Increase the DURATION of GABA mediated chloride ion channels
Barbiturate used for the induction of anesthesia
Thiopental
Site of action of Zaleplon Zolpidem
Benzodiazepine receptopr BZ1 (although do no have a benzodiazepine ring structure)
Good hypnotic activity with less CNS SE than most Benzodiazepines
Zolpidem
Zaleplon
Agent that is a partial agonist to the 5-HT1a receptor
Buspirone
DOC for Generalized Anxiety Disorder, NOT effective in acute anxiety
Buspirone
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Ethanol
*
Agent with zero-order kinetics
Ethanol
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
System that increased in activity with chronic ethanol exposure and may contribute to tolerance
MEOS
*
Enzyme that metabolizes acetaldehyde to acetate
Aldehyde Dehydrogenase
Agents that inhibit acetaldehyde dehydrogenase (~4)
Disulfram
Metronidazole
Certain Sulfonylureas
Certain Cephalosporins
Agent that inhibits alcohol dehydrogenase and its clinical use
Fomepizole

used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
Disulfram
The most common neurologic abnormality in chronic alcoholics
Peripheral Neuropathy (also htn, anemia, mi)
*
Agent that is teratogen and causes a fetal syndrome
Ethanol
Agent that is the antidote for methanol overdose
Ethanol and Fomepizole
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Fomepizole
Most frequent route of metabolism for anti-seizure drugs
Hepatic enzymes
MOA for Phenytoin, Carbamazepine, Lamotrigine
Sodium Channel blockade
MOA for benzodiazepines and barbituates
GABA-related targets
MOA for Ethosuximide
Calcium Channels
MOA for Valproic Acid @ high doses
Affect Ca/K/Na Channels
DOC(2) for generalized tonic-clonic and partial seizures
Valproic Acid
Phenytoin
*
DOC for Febrile Seizures
Phenobarbital
DOC (2) for absence seizures
Ethosuximide
Valproic Acid
*
DOC for myoclonic seizures
Valproic Acid
*
DOC for status epilepticus
IV Diazepam (acute)
Phenytoin prolonged
Drugs that can be used for infantile spasms
Corticosteroids
Anti-seizure drugs used also for bipolar affective disorder (BAD) (4)
Valproic Acid
Carbamazepine
Phenytoin and
Gabapentin
Anti-seizure drugs also used in Trigeminal Neuralgia
Carbamazepine
Anti-seizure drugs used also for pain of neuropathic origin
Gabapentin
*
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
Phenytoin
SE of Phenytoin
Gingival hyperplasia
Nystagmus
Diplopia
Ataxia
*
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogenic, and can cause craniofacial anomalies and spina bifida
Carbamazepine
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defecs and GI distress
Valproic Acid
Laboratory value required to be monitored for patients on valproic acid
Serum Ammonia and LFTs
SE for Lamotrigine
SJS
SE for Felbamate
Aplastic Anemia and Acute Hepatic Failure
Anti-seizures medication also used in the prevention of migraines
Valproic Acid
Carbamazepine may cause
Agranulocytosis
Anti-seizure drugs used as -alternative drugs- for mood stabilization (4)
Carbamazepine
Gabapentin
Lamotrigine
Valproic Acid
MOA of general anesthetics
Most are thought to act at GABA-A receptor Chloride Channel
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous Oxide
Inversely related to potency of anesthetics
Minimum Alveolar Anesthetic Concentration (MAC)
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents (2)
Halothane
Methoxyflurane
Most inhaled anesthetics SE
Decreased arterial blood pressure
Inhaled anesthetics which are myocardial depressants (2)
Enflurane
Halothane
Inhaled Anesthetic which causes peripheral vasodilation
Isoflurane
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Halothane
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect of respiration
Nitrous Oxide
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Methoxyflurane
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
Nitrous Oxide
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
Desflurane
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
Dantrolene
*
IV barbiturate used as a pre-op anesthetic
Thiopental
Barbiturate used adjunctively in anesthesia
Midazolam
Benzodiazepine receptor antagonist, accelerates recovery from benzodiazepine overdose
Flumazenil
*
This produces a "dissociative anesthesia", is a cardiovascular stimulant which may increase intracranial pressure, and hallucinations occur during recovery
Ketamine
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthesia
Fentanyl
*
State of analgesia and amnesia produced when Fentanyl is used with Droperidol and Nitrous Oxide
Neuroleptanesthia
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
Propofol
MOA of LA (Local Anesthetics)
Block voltage-dependent sodium channels
This may enhance activity of local anesthetics
Hyperkalemia
This may antagonize activity of LAs
Hypercalcemia
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex - epinephrine) to prolong activity
Vasodilation
LA with vasoconstrictive properties favored for head, neck, and pharyngeal surgery
Cocaine
Longer acting LAs which are less dependent on vasoconstrictors (2)
Tetracaine
Bupivacaine
These LAs have surface activity (2)
Cocaine
Benzocaine
Most important toxic effects of most local anesthetics
CNS toxicity
Commonly abused LA which has cardiovascular toxicity including severe HTN with cerebral hemorrhage, cardiac arrhythmias, and MI
Cocaine
LA causing methemoglobinemia
Prilocaine
Structurally related to Acetylcholine, used to produce muscle paralysis in order to facilitate surgery of artificial ventilation. Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
These drugs strongly potentiate and prolong effect of NMB (Neuromussular blockade)
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmics
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade", effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
Nondepolarizing type antagonists
Agent with long duration of action and is most likely to cause histamine release
Tubocurarine
Non-depolarizing skeletal muscle antagonist that has short duration
Mivacurium
Skeletal muscle agent that can block muscarinic receptors
Pancuronium
Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
Atracurium
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
Succinylcholine
During Phase I these agents worsen muscle paralysis by succinylcholine, but during Phase II they reverse the blockade produced by succinylcholine
Cholinesterase Inhibitors
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
Spasmolytic Drugs
Facilitates GABA presynaptic inhibition
Diazepam
GABA agonist in the spinal cord
Baclofen
Similar to Clonidine and may cause hypotension
Tizanidine
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum of skeletal muscle
Dantrolene
*
Agent used for acute muscle spasm
Cyclobenzaprine
Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
Drug induced Parkinsonism
*
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
L-dopa
This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
Carbidopa
Clinical response that may fluctuate in treatment of Parkinson's Disease
On-Off Phenomenon
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
Levodopa
Ergot Alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate Levodopa, causes erythromelaglia
Bromocriptine
Non ergot agents used as first-line therapy in the initial management of Parkinson's (2)
Pramipexole
Ropinirole
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis, and livedo reticularis
Amantadine
Inhibitor of MAO type B which slows down metabolism of Dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
Selegiline
Inhibitors of Catechol-O-Methyltransferase (COMT), used as adjuncts in Parkinson's Disease and cause acute hepatic failure (monitor LFTs)
Tolcapone
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like SEs
Benztropine
Agent effective in physiologic and essential tremor
Propranolol
Agents used in Huntington's Disease (2)
Tetrabenazine (amine depleting drug)
Reserpine
Agents used in Tourette's Dz (3)
Haloperidol
Pimozide
Clonidine
Chelating agent used in Wilson's Disease
Penicillamine
ANTIPSYCHOTICS
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
Older Antipsychotic agents, D2 receptors
ANTIPSYCHOTICS
MOA of Neuroleptics
Dopamine blockade
ANTIPSYCHOTICS

SEs occuring in antipsychotics that block dopamine (7)
Hyperprolactinemia
Menorrhea
Galactorrhea
Confusion
Mood Changes
Decreased Sexual Interest
Weight Gain
*
ANTIPSYCHOTICS

Antipsychotics that reduce positive symptoms only
Older Antipsychotics
ANTIPSYCHOTICS
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation (3)
Olanzapine
Aripiprazle
Sertindole
ANTIPSYCHOTICS

Antipsychotic used in treatment of psychiatric symptoms in patients with dementia
Risperidone
*
ANTIPSYCHOTICS
Atypical antipsychotic causing high prolactin levels
Risperidone
*
ANTIPSYCHOTICS
Newer Atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
Olanzapine
ANTIPSYCHOTICS
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine, or muscarinic blocker
Haloperidol
ANTIPSYCHOTICS
Drug used in neuroleptic malignant syndrome
Dantrolene
*
ANTIPSYCHOTICS
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
Muscarinic Blockers
ANTIPSYCHOTICS
Antipsychotic having the strongest autonomic effects
Thioridazine
*
ANTIPSYCHOTICS
Antipsychotic having the weakest autonomic effects
Haloperidol
ANTIPSYCHOTICS
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
Thioridazine
ANTIPSYCHOTICS
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schiophrenia, and can cause fatal agranulocytosis
Clozapine
**
ANTIPSYCHOTICS
Antipsychotic not shown to cause Tardive Dyskinesia
Clozapine
*
ANTIPSYCHOTICS
antipsychotic available in a depot preparation (2)
Fluphenazine
Haloperidol
ANTIPSYCHOTICS
Reduced seizure threshold
Low-potency typical antipsychotics and clozapine
ANTIPSYCHOTICS
Orthostatic HTN and QT prolongation
Low potency phenothiazines and ziprasidone
ANTIPSYCHOTICS
Increased risk of developing cataracts
Quetiapine
LITHIUM
Major route of elimination
Kidneys
*
LITHIUM
Patients being treated with lithium, who are dehydrated or taking diuretics concurrently, could develop
Lithium toxicity
*
LITHIUM
Drug increases the renal clearance hence decreases levels of lithium
Theophylline
LITHIUM
Associated with this congenital defect
cardiac anomalies and is contraindicated in pregnancy and lactation
DOC for bipolar affective disorder
Lithium
*
LITHIUM
Concern using lithium
Low therapeutic index
LITHIUM
SEs (6)
Tremor
Sedation
Ataxia
Aphasia
Thyroid Enlargement
Reversible Diabetes Insipidus
ANTIDEPRESSANTS
Example of 3 indicated for OCD
Clomipramine
Fluoxetine
Fluvoxamine
ANTIDEPRESSANTS
Neurotransmitters affected by the action of antidepressants
Norepinephrine and Serotonin
ANTIDEPRESSANTS
Usual time needed for full effect
2 to 3 weeks
ANTIDEPRESSANTS
Population group especially sensitive to SEs
Elderly
ANTIDEPRESSANTS
All have roughly the same efficacy in treating depression, agents chosen based on these criterion (2)
SE profile
Prior pt response
ANTIDEPRESSANTS
Well-tolerated and are first-like antidepressants
SSRIs
Bupropion
Venlafaxine
ANTIDEPRESSANTS
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant antidepression
MOAIs
ANTIDEPRESSANTS
Condition will result from in combination of MAOI with Tyramine containing foods (wine, cheese, pickled meats)
Hypertensive Crisis
ANTIDEPRESSANTS
MAOI should not be administered with SSRIs or potent TCAs due to the development of
Serotonin Syndrome
ANTIDEPRESSANTS
Sedation is a common SE of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
TCAs
ANTIDEPRESSANTS
Three C's associated with TCA toxicity
Come
Convulsions
Cardiac (arrhythmias and wide QRS)
ANTIDEPRESSANTS
Agents having higher sedation and antimuscarinic effects than other TCAs
Tertiary amines
ANTIDEPRESSANTS
TCA used in chronic pain, a hypontic, and has marked antimuscarinic effects
Amitriptyline
ANTIDEPRESSANTS
TCA used in chronic pain, enuresis, and ADD
Imipramine
*
ANTIDEPRESSANTS
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
Doxepin
ANTIDEPRESSANTS
TCA used in OCD, most signification of TCAs for risk of seizures, weight gain, and neuropsychiatric sign and symptoms
Clomipramine
ANTIDEPRESSANTS
Secondary Amines that have less sedation and more excitation effect (2)
Nortiptyline
Desipramine
ANTIDEPRESSANTS
SEs seen with TCAs
Muscarinic Blockade causes constipation and dry mouth
Weak a1 block causes orthostatic hypotension
Weak Histamine block causes sedation
ANTIDEPRESSANTS
Antidepressant associated with neuroleptic malignant syndrome
Amoxapine (Heterocyclic)
ANTIDEPRESSANTS(Heterocyclics)
Antidepressant associated with seizures and cardiotoxicity
Maprotiline
ANTIDEPRESSANTS(Heterocyclics)
Antidepr. having stimulant effects similar to SSRIs and can increase blood pressure
Venlafaxine
ANTIDEPRESSANTS(Heterocyclics)
Antidepressant inhibiting NE, Serotonin, and Dopamine reuptake
Venlafaxine
ANTIDEPRESSANTS
Antidepr. also used for sleep that causes priapism
Trazodone (heterocyclic)
ANTIDEPRESSANTS
inhibitor of CYP450 enzymes and may be associated with hepatic failure
Nefazodone (hetercyclic)
ANTIDEPRESSANTS
Heterocyclic antidepr. least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
Bupropion
*
ANTIDEPRESSANTS
antidepr with MOA as alpha2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
Mirtazapine
ANTIDEPRESSANTS
SE of Mirtazapine
Liver Toxicity, increased serum cholesterol
ANTIDEPRESSANTS
Except for these agents all SRRI have significant inhibition of CYP450s
Citalopram and its metabolite escitalopram
ANTIDEPRESSANTS
SEs frequently seen with SSRIs (2)
CNS Stimulation
GI Upset
ANTIDEPRESSANTS
Antidepr with no effect on BP, no sedation
SSRIs
ANTIDEPRESSANTS
SSRI with long t1/2 and can be administered once weekly for maintenance, no acute treatment
Fluoxetine
ANTIDEPRESSANTS
SSRI indicated for premenstrual dysphoric disorder
Fluoxetine (Sarafem)
ANTIDEPRESSANTS
Some of SSRI's therapeutic effects besides depression (5)
Panic Attacks
Social Phobias
Bulimia Nervosa
PMDD
OCD
ANTIDEPRESSANTS
SSRI less likely to cause a withdrawal syndrome
Fluoxetine
OPIOID ANALGESICS/ANTAGONISTS
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
Ascending pathways
OPIOID ANALGESICS/ANTAGONISTS
Activation of these receptors close Calcium Ion Channels to inhibit neurotransmitter release
Presynaptic Mu/delta/kappa receptors
*
OPIOID ANALGESICS/ANTAGONISTS
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
Postsynaptic Mu receptors
OPIOID ANALGESICS/ANTAGONISTS
Tolerance to all effects of opioid agonists can develop except
miosis
constipation
*
OPIOID ANALGESICS/ANTAGONISTS
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
Meperidine
OPIOID ANALGESICS/ANTAGONISTS
SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression, N/V/Constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
Opioid Analgesics
OPIOID ANALGESICS/ANTAGONISTS
Strong opioid agonists (4)
Morphine
Methadone
Meperidine
Fentanyl
OPIOID ANALGESICS/ANTAGONISTS
Opioids used in anesthesia (2)
Morphine
Fentanyl
OPIOID ANALGESICS/ANTAGONISTS
Opioid used in the management of withdrawal states
Methadone
*
OPIOID ANALGESICS/ANTAGONISTS
Opioid available trans-dermally
Fentanyl
*
OPIOID ANALGESICS/ANTAGONISTS
Opioid that can be given PO, epidural, and IV which helps to relieve the dyspnea of Pulmonary Edema
Morphine
*
OPIOID ANALGESICS/ANTAGONISTS
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRIs can lead to serotonin syndrome
Meperidine
OPIOID ANALGESICS/ANTAGONISTS
Moderate Opioid Agonists (3)
Codeine
Hydrocodone
Oxycodone
*
OPIOID ANALGESICS/ANTAGONISTS
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema and seizures
Propoxyphene
OPIOID ANALGESICS/ANTAGONISTS
Partial agonist, considered analgesic, has a long duration of action and is resistant to Naloxone reversal
Buprenophrine
OPIOID ANALGESICS/ANTAGONISTS
Opioid antagonist that is given IV and has short DOA
Naloxone
OPIOID ANALGESICS/ANTAGONISTS
Opioid antagonist that is given orally in alcohol dependency programs
Naltrexone
*
OPIOID ANALGESICS/ANTAGONISTS
These agents are used as antitussive (2)
Dextromethorphan
Codeine
OPIOID ANALGESICS/ANTAGONISTS
These agents are used as antidiarrheals (2)
Diphenoxylate
Loperamide
DRUGS OF ABUSE
Inhalant Anesthetics
NO
Chloroform
Diethyl Ether
DRUGS OF ABUSE
Toxic to liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
Fluorocarbons
Industrial Solvents
DRUGS OF ABUSE
Cause dizziness, tachycardia, hypotension, and flushing
Organic Nitrites
DRUGS OF ABUSE
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
Steroids
DRUGS OF ABUSE
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include:
Changes in heart rate, blood pressure, respiration, temperature, sweating, bowel signs, pupillary responses
*
OPIOID ANALGESICS
Most commonly abused in heatlh care professionals? (5)
Heroin
Morphine
Oxycodone
Meperidine
Fentanyl
OPIOID ANALGESICS
This route is associated with rapid tolerance and psychologic dependence
IV administration
OPIOID ANALGESICS
Leads to respiratory depression progressing to coma and death
Overdose of Opioids
OPIOID ANALGESICS
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
Abstinence Syndrome
OPIOID ANALGESICS
Treatment of Opioid addiction
Methadone, followed by slow dose reduction
OPIOID ANALGESICS
This agent many cause more severe, rapid and intense symptoms to a recovering addict
Naloxone
*
Sedative-Hypnotics

Action
Reduce inhibition, supress anxiety, and produce relaxation
Sedative-Hypnotics

Additive effects when Sedative-Hypnotics used in combination with these agents
CNS depressants
Sedative-Hypnotics

Common mechanism by which overdose results in death
depression of medullary and cardiovascular centers
"Date Rape drug"
Flunitrazepam (Rohypnol)
*
Sedative-Hypnotics

most important sign of withdrawal syndrome
Excessive CNS stimulation (seizures)
Sedative-Hypnotics

treatment of withdrawal syndrome involves
Long-acting Sedative-Hypnotic or a gradual reduction of dose, clonidine or propranolol
Sedative-Hypnotics

These agents are CNS depressants
Ethanol, barbituates, and benzodiazepines
*
Stimulants

Withdrawal from this drug causes lethargy, irritability, and headache
Caffeine
Stimulants

W/D from this drug causes anxiety and mental discomfort
Nicotine
Stimulants

Treatments available for nicotine addiction
Patches
Gum
Nasal Spray
Psychotherapy
Bupropion
*
Stimulants

Chronic high dose abuse of nicotine leads to
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
Stimulants

Tolerance is marked and abstinence syndrome occurs
Amphetamines
Stimulants

Amphetamine agents
Dextroamphetamines
Methamphetamine
Stimulants

These agents are congeners of Amphetamine
DOM
STP
MDA
MDMA "Ecstacy"
Stimulants
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and Stroke)
Cocaine "super-speed"
Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked HTN, and seizures. Presence of both horizontal and vertical is pathognomonic
PCP
Removal of PCP may be aided
Urinary acidification and activated charcoal or continual nasogastric suction
THC is active ingredient, SE's include impairment of judgement and reflexes, decreases in blood pressure, and psychomotor performance occur
Marijuana
*
Direct-acting Cholinomimetic Agonists

This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
Bethanechol
*
Direct-acting Cholinomimetic Agonists

Only direct acting agent that is very lipid soluble and used in glaucoma
Pilocarpine
This agent used to treat dry mouth in Sjogren's Syndrome
Cevimeline
Indirect-acting Ach agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
Edrophonium
Carbamate with intermediate action, used for +A1170 postoperative and neurogenic ileus and urinary retention
Neostigmine
Treatment of atropine overdose and glaucoma (because lipid soluble). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
Physostigmine
Treatment of Myasthenia Gravis
Pyridostigmine
Antiglaucoma organophosphate
Echothiophate
Associated with an increased incidence of cataracts in patients treated for glaucoma
LA Cholinesterase inhibitors
Scabicide Organophosphate
Malathion
Organophosphate anthelmintic agent with long DOA
Metrifonate
Toxicity of Organophosphate
DUMBELSS
Diarrhea, urination, miosis, bronchoconstriction, excitation of SkM/CNS, Lacrimation, Salivation, and Sweating
*
The most frequent cause of acute deaths in cholinesterase inhibitor toxicity
Respiratory failure
The most toxic organophosphate
Parathion
Treatment of choice for organophosphate overdose
Atropine
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
Pralidoxime
Prototypical drug is atropine
Nonselective muscarinic antagonists
Treatment manifestations of Parkinson's Disease and EPS
Benztropine
Trihexyphenidyl
*
Treatment of Motion Sickness
Scopolamine
Meclizine
*
Cholinoreceptor blockers & Cholinesterase Regenerators

Produce mydriasis and cycloplegia (3)
Atropine
Homatropine
C1208 Tropicamide
*
Cholinoreceptor blockers & Cholinesterase Regenerators

Bronchodilation in asthma and COPD
Ipratropium
*
Cholinoreceptor blockers & Cholinesterase Regenerators

Reduce transient hyper GI motility
Dicyclomine
Methscopolamine
Cholinoreceptor blockers & Cholinesterase Regenerators

Cystitis, postoperative bladder spasms, or incontinence (2)
Oxybutynin
Dicyclomine
Toxicity of anticholinergics
Block SLUD (salivation, lacrimation, urination, defecation)
Antother pneumonic for anticholinergic toxicity
Dry as a bone
Red as a beet
Mad as a hatter
Hot as a hate
Blind as a bat
Atropine fever is the most dangerous effect and can be lethal in this population group
Infants
Contraindications to the use of atropine (3)
Infants
Closed angle glaucoma
Prostatic hypertrophy
Nicotinic Antagonists

Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
Severe HTN
Nicotinic Antagonists

Reversal of blockade by neuromuscular blockers
Cholinesterase inhibitors
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agents, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
Nondepolarizing neuromuscular blockers
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use; has short DoA
Succinylcholine
Chemical antagonists that bind to the inhibitor of ACh estrace and displace the enzyme (if aging has not occurred)
Cholinesterase regenerators, pralidoxime
Used to treat patients exposed to insecticides such as parathion
Pralidoxime
Atropine
Pneumonic for beta receptors
You have 1 Heart (Beta 1) and 2 lungs (Beta 2)
*
This is the DOC for anaphylactic shock
Epinephrine
*
Phenylisopropylamines that are used legitimately and abused for narcolepsy, ADD, and weight reduction
Amphetamines
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
Phenylephrine
Newer alpha 2 agonist (apraclonidine and brimonidine)
Reduce aqueous secretion
Short acting Beta2 agonist that is DOC in treatment of acute asthma but not recommended for prophylaxis
Albuterol
Longer acting Beta2 agonist is recommended for prophylaxis of asthma
Salmeterol
These agents increase cardiac output and may be beneficial in treatment of acute heart failure and some types of shock
Beta1 Agonists
These agents decrease blood flow or increase blood pressure, are local decongestants, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion)
Alpha1 agonist
*
Shock due to septicemia or MI is made worse by
Increasing afterload and tissue perfusion declines
Epinephrine is often mixed with a local anesthetic to
Reduce the loss from area of injection
Chronic orthostatic hypotension can be treated with
Midodrine
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
Terbutaline
Sympathetic agent which stimulates heart rate and can dilate vessels in skeletal muscle at low doses
Epinephrine
Mast cells to reduce release of histamine and inflammatory mediators
Epinephrine
Agent used in shock because is dilates coronary arteries and increases renal blood flow
Dopamine
Agent which stimulates cardiac contractile force more than rate with little effect on total peripheral resistance
Dobutamine
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
Ephedrine
Alpha 1 agonist toxicity
HTN
*
Beta 1 agonist toxicity
Sinus tachycardia and serious arrhythmias
Beta 2 agonist toxicity
Skeletal muscle tremor, tachycardia
The selective agents loose their selectivity at
high doses
Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionally used for carcinoid tumor. Blocks H1 and used in mastocytosis
Phentolamine
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension (3)
Prazosin
Terazosin
Doxazosin
*
Selective Alpha 1A blocker used for BPH, but with little effect on HTN
Tamsulosin
Selective Alpha 2 blocker used for impotence (controversial effectiveness)
Yohimbine
Selective B1 receptor blockers that may be useful in treating patients even though they have asthma (4)
Acebutolol
Atenolol
Esmolol
Metoprolol
*
Combined alpha and beta blocking agents that may have application in treatment of CHF (2)
Labetalol and Carvedilol
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma (2)
Pindolol
Acebutolol
This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
Timolol
*
This parenteral beta blocker is short acting
Esmolol
This beta blocker is the longest acting
Nadolol
These beta blockers are less lipid soluble (2)
Acebutolol
Atenolol
This beta blocker is highly lipid soluble and may account for SEs such as nightmares
Propanolol
Clinical uses of these agents include treatment of HTN, angina, arrhythmias, chronic CHF, and selected post MI patients
Beta Blockers
Toxicity of these agents include bradycardia, AV blockage, exacerbation of acute CHF; signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety)
Beta Blockers
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliar muscle contraction (3)
Pilocarpine
Carbachol
Physostigmine
Nonselective alpha agonist that increases outflow, probably via the uveoscleral veins (2)
Epinephrine
Dipivefrin
Selective alpha agonists that decrease aqueous secretion (2)
Apraclonidine
Brimonidine
These beta blockers decrease aqueous secretion (2)
Timolol (nonselective)
Betaxolol (Selective)
*
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis
Acetazolamide
This agent causes increased aqueous outflow
PGF2a
Inhibit ACE
ACE inhibitors
*
Captopril and enalapril (-OPRIL ending) are
ACE inhibitors
*
SE of ACE inhibitors
Dry Cough
Hyperkalemia
*
ACE inhibitors are contraindicated in
pregnancy
with K+
*
Losartan and Valsartan block
Angiotensin receptor
*
Angiotensin receptor blockers do NOT cause
Dry cough
*
Agents that block L-type calcium channel
Calcium channel blockers
CCB containdicated in CHF
Verapamil
*
CCB with predominate effect on arteriole dilation
Nifedipine
SE of CCB
Constipation
Edema
Headache
*
Agents that reduce heart rate, contractility, and O2 demand
Beta Blockers
*
Beta Blockers that are more cardioselective
Beta 1 selective blockers
Cardioselective B1 blockers (3)
Atenolol
Acebutolol
Metoprolol
*
Beta blockers should be used cautiously in
Asthma (bronchospastic)
Diabetes (block signs of hypoglycemia)
Peripheral Vascular Disease
Nonselective beta blocker also used for migraine prophylaxis
Propanolol
SE of beta blockers
Bradycardia
SEXUAL DYSFUNCTION
Decrease in HDL
Increase in TGs
*
Alpha1 selective blockers (3)
Prazosin
Terazosin
Doxazosin
(AZOSIN endings)
*
Nonselective alpha1 blockers use to treat pheochromocytoma
Phenoxybenzamine
For rebound HTN from rapid clonidine withdrawal
Phentolamine
A1a selective blocker with no effects on HTN used for BPH
Tamsulosin (Flomax)
*
SE of alpha blockers
Orthostatic hypotension (especially with first dose)
Reflex Tachycardia
*
Presynaptic alpha2 agonist used in HTN, and acts centrally (2)
Clonidine
Methyldopa
SE of methyldopa
Positive Coomb's test (tests for autoimmune hemolytic anemia)
Depression
Methyldopa is contraindicated in
Geriatrics due to its CNS depression effects
SE of Clonidine
Rebound HTN
Sedation
Dry Mouth
Direct vasodilator of arteriolar smooth muscle
Hydralazine
SE of Hydralazine
Lupus-like syndrome
*
Arterial vasodilator that works by opening K+ channels
Minoxidil
SE of minoxidil
Hypertrichosis
IV drug used in hypertensive crisis
Nitroprusside
Nitroprusside vasodilates
arteries and veins
toxicity caused by nitroprusside and treatment
Cyanide toxicity treated with sodium thiosulfate
Carbonic anhydrase inhibitor
Acetazolamide
Diuretic used for mountain sickness and glaucoma
Acetazolamide
*
SE of Acetazolamide
Paresthesias
Alkalization of urine (may ppt Ca salts)
Hypokalemia
Acidosis
Encephalopathy in patients with hepatic impairment
*
MOA of Loop Diuretics
Inhibits Na/K/2Cl contransport
Site of action of loop diuretics
Thick ascending limb
*
SE of loop (furosemide) diuretics
Hyperuricemia
Hypokalemia
Ototoxicity
*
Aminogylcosides used with loop diuretics potentiate adverse effect
Ototoxicity
Loops lose and thiazide diuretics retain
Calcium
*
MOA of thiazide diuretics
Inhibit Na/Cl cotransport
Site of action of thiazide diuretics
early DCT
*
Class of drugs that may cause cross-sensitivity with thiazide diuretics
Sulfonamides
SE of thiazide (HCTZ) diuretics (3)
Hyperuricemia
Hypokalemia
Hyperglycemia
*
Potassium sparing diuretics inhibit
Na/K exchange
*
Diuretic used to treat primary aldosteronism
Spironolactone
*
SE of spironolactone (3)
Gynecomastia
Hyperkalemia
Impotence
*
Osmotic Diuretic used to treat increased intracranial pressure
Mannitol
*
ADH agonist used for pituitary diabetes insipidus
Desmopressin (DDAVP)
Used for SIADH
Demeclocycline
SE of Demeclocycline
Bone marrow and teeth discoloration for children under 8 years of age
MOA of class 1a (eg procainamide), class 1b (eg lidocaine), and class 1c (eg Flecainide) antiarrhythmics
Sodium Channel Blockers
*

is this true?
SE of Procainamide
Lupus-like syndrome
Limiting SE of Quinidine
Prolongs QT interval
*
Other SEs of Quinidine
Thrombocytopenic Purpura
CINCHONISM
Major drug interaction with Quinidine
Increases concentration of Digoxin
DOC for management of acute ventricular arrhythmias
Amiodarone
*
DOC for digoxin induced arrhythmias
Phenytoin
SE of Phenytoin
Gingival Hyperplasia
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as -last- line agents
Class 1C (Flecainide, propafenone, moricizine)
Class II antiarrhytmics are
Beta blockers
Antiarrhythmic that exhibits Class II and Class III properties
Sotalol
SE of Sotalol
prolongs QT and PR interval
Used IV for acute arrhythmias during surgery
Esmolol
Anti-arrhythmics that decrease mortality
Beta blockers
MOA of class III antiarrhythmics
K+ channel blockers
Class III antiarrhytmic that exhibits properties of all 4 classes
Amiodarone