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273 Cards in this Set

  • Front
  • Back
Trimethoprim
Antibiotic
Anti-metabolite
Bacteriostatic
Inhibits dihydrofolate reductase
Synergy w/ sulfonamides
Used alone for G- UTI
Sulfonamides
Antibiotic
Anti-metabolie
Bacteriostatic
Inhibits dihydropteroate synthetase
Synergy w/ trimethoprim
Broad spectrum

Uses: UTI, chlamydia (oral), ulcerative colitis, comatose meningitis (IV)

Nephrotoxicity, hemolysis, Stevens-Johnson rxn, crystalluria
Pregnancy!
Penicillin + Tetracylines
Bad!
Bactericidal + bacteriostatic
Penicillin + Aminoglycoside
Prophylaxis & mixed infections
Aminoglycoside allows the penicillin to get in
Isoniazid + Rifampin
TB
Trimethoprim + Sulfamexazole
Pneumocystis carinii pneumonia (HIV)
Sulfonamides + Trimethoprim
Synergy together
Two bacteriostatics together
Penicillins
Antibiotics
Cell-Wall Synthesis Inhibitors
Block transpeptidase reaction (binds PBPs)
Excreted
Gram+ (except broad-spectrum ones)
ONLY active against dividing bacteria

Least toxic, most allergenic
Penicillin G - neurotoxicity
Penicillin Resistance
Beta-lactamases (penicillinases) cleave the beta-lactam ring

Penicillin-Binding Proteins less responsive
Cephalosporins
Antibiotics
Cell-Wall Synthesis Inhibitors
Treat klebsiella
Gram- and gram
+
No repository form
Block transpeptidase reaction

Allergy, bleeding disorders (reverse with Vit K)
Alcohol (disulfiram disorders)
Vancomycin
Antibiotic
Cell-Wall Synthesis Inhibitor
Bactericidal
C. diff (oral), MRSAs
Bone & CSF
IV for everything other than C. diff
80% excreted
Narrow spectrum: strep, pneumo, staph, some anaerobes

Flushing (histamine), ototoxicity, nephrotoxicity
Bacitracin
Antibiotic
Cell-Wall Synthesis Inhibitor
C. diff (oral), topical (little absorbed this way)
Gram+

Nephrotoxic
Cycloserine
Antibiotic
Cell-Wall Synthesis Inhibitor
Blocks alanine racemase
Rifampin
Antibiotic
Nucleic Acid Inhibitor
Inhibits RNA polymerase

Birth control pills, other drugs (enhances breakdown)
Ciprofloxacin
Antibiotic
Quinolone

Blocks DNA gyrase

Metronidazole
Antibiotic (antiparasitic)
Nucleic Acid Inhibitor
Blocks synthesis of nucleic acids (bactericidal)
C. diff (1st choice)! Preop, endocarditis
Obligate anaerobes ONLY

GI, carcinogenic, alcohol (disulfiram-like reaction)
Isoniazid
Antibiotic

Liver toxicity
All antibiotics
GI toxicity
Cross-sensitivity can occur; they act as haptens
Polymyxins
Antibiotic
Cell Membrane Affector
Bind phosphatidyl ethanolamine rich areas
Form pores in cell membranes
Gram-
Oral (g- in gut), IM (UTIs), topical (w/ bacitracin/neomycin)

Nephrotoxicity (phosphatidyl ethanolamine in kidney)
Cholistins
Newer polymyxins
Less toxic
Chloramphenicol
Antibiotic
Protein Synthesis Inhibitor
Binds 50S; inhibits chain elongation
Bacteriostatic
G-
Salmonella, typhoid fever, rickettsia (Rocky Mountain Spotted Fever)

Inhibits P450, toxic to marrow, hemolysis (red cell anemia)
Phenytoin & cumadin (P450); pregnancy
Erythromycin
Antibiotic
Protein Synthesis Inhibitor
Binds 50S; inhibits chain elongation
Clindamycin
Antibiotic
Protein Synthesis Inhibitor
Binds 50S; inhibits chain elongation; bacteriostatic & bactericidal
Oral; excreted in bile
Broad spectrum; g+ & g-

Uses: G+ bone infx; anaerobic pneumonia; MRSAs; strep, staph, bacteriodes

Causes C. diff!
Tetracyclines
Antibiotics
Protein Synthesis Inhibitors
Block tRNA from binding 30S
Bacteriostatic
Oral
Well-distributed

Uses: mycoplasma, chlamydia, rickettsia (1st choice Rocky Mountain Spotted Fever), severe acne

Hepatotoxicity, neurotoxicity
Pregnancy
Aminoglycosides
Antibiotics
Bind to 30S, inhibit protein synthesis
Bactericidal
Parenteral, good bone penetration
Broad spectrum; mainly against G-

Nephrotoxicity, neurotoxicity (auditory/vestibular)
Streptomycin
Antibiotic
Aminoglycoside
TB, mycobacterial, non-TB infections
Endocarditis (w/ penicillin)

Pregnancy (CN VIII damage; skeletal defects)
Dicloxacillin
Antibiotic
Penicillinase-Resistant Penicillin
Oxacillin
Antibiotic
Penicillinase-Resistant Penicillin
Nafcillin
Antibiotic
Penicillinase-Resistant Penicillin
Cloxacillin
Antibiotic
Penicillinase-Resistant Penicillin
Penicillin G
Antibiotic
All routes
Repository - syphilis
Penicillin V
Antibiotic
Oral only
Ampicillin
Antibiotic
Broad-Spectrum Penicillin
Kills gram- b/c of lipophilic side chains
G- meningitis
Carbenicillin
Antibiotic
Broad-Spectrum Penicillin
Kills gram- b/c of lipophilic side chains
Pseudomonas, ampicillin-resistant bacteria
Clavulanic Acid
Beta-Lactamase Inhibitor
Potentiates antibiotics by preventing breakdown
Sulbactam
Beta-Lactamase Inhibitor
Potentiates antibiotics by preventing breakdown
Tazobactam
Beta-Lactamase Inhibitor
Potentiates antibiotics by preventing breakdown
Imipenem
Antibiotic
Carbapenem
Serious infections

Seizures
Use with cilastatin (stops its metabolism)
Azteronam
Antibiotic
Monobactam
Kills gram- only (pseudomonas, serratia, E. coli)
3rd Gen Cephalosporins
Antibiotic
Gram- meningitis (gets into CSF), gonorrhea
2nd Gen Cephalosporins
Antibiotic
Penicillin-resistant bacteria
Cefepime
Antibiotic
4th Gen Cephalosporin
4th Gen Cephalosporins
Antibiotic
Haemophilus, neisseria
Penetrates CSF
Cefazolin
Antibiotic
1st Gen Cephalosporin
1st Gen Cephalosporins
Antibiotic
Surgery prophylaxis
Inexpensive
Cephalosporin Resistance
Cephalosporinases (like penicillinases)
Can use against penicillin-resistant bacteria!
Macrolides
Antibiotics
Concentrated in liver (excreted in bile)
G+
Erythromycin, semi-synthetic erythromycins
Bind 23S RNA of 50S subunit

Uses: 1st choice mycoplasma, alt. to penicillin G, Legionnaire's, pneumonia, chlamydia, rickettsia
Clarithromycin
Antibiotic
Macrolide (G+); Semi-Synthetic Erythromycin
Broader spectrum, better permeability

Inhibits P450
Azithromycin
Antibiotic
Macrolide (G+); Semi-Synthetic Erythromycin
Broader spectrum, better permeability
Long half-life (3 days)
Penetrates more at low serum level

Does NOT inhibit P450
Erythromycin
Antibiotic
Macrolide (G+)

Inhibits P450
Macrolide Resistance
Ribosomes don't bind it
Never use alone for bad staph infection
Clindamycin Resistance
Subunit stops binding
Dificid
Antibiotic
C. diff
Vancomycin Resistance
If resistant, treat with tigecycline/synercid/linezolid
Tigecycline
Antibiotic
Vancomycin-resistant bacteria
Synercid
Antibiotic
Vancomycin-resistant bacteria
Mix of 2 bacteriostatics
Linezolid
Antibiotic
Vancomycin-resistant bacteria
Inhibits protein synthesis
Amikacin
Antibiotic
Aminoglycoside
Resistant to enzymes (resistance)
Broadest spectrum
Aminoglycoside Resistance
Metabolized by bacteria enzymes
Kanamycin
Antibiotic
Aminoglycoside
Topical, oral (reduce gut flora before surgery)
Neomycin
Antibiotic
Aminoglycoside
Topical, oral (reduce gut flora before surgery)
Gentamycin
Antibiotic
Aminoglycoside
IM, topical, intrathecal (G- meningitis)
Tobramycin
Antibiotic
Aminoglycoside
IM, topical, intrathecal (G- meningitis)
Netilmicin
Antibiotic
Aminoglycoside
IM, topical, intrathecal (G- meningitis)
Spectinomycin
Antibiotic
Aminoglycoside
IM
Gonorrhea in penicillin-allergic
Sulfasalazine
Antibiotic
Sulfonamide
Ulcerative colitis
Sulfanilamide
Antibiotic
Sulfonamide
Inhibit PABA (needed for bacteria to make folate)
Sulfamethoxazole
Antibiotic
Sulfonamide
Oral, sodium salt IV, topical
Sulfonamide Resistance
Enzyme binds drug less (dihydropteroate synthetase)
Nitrofurantoin
Antibiotic
Urinary Antiseptic (pH <5.5)
Methenamine Mandelate
Antibiotic
Urinary Antiseptic (ph <5.5)
Release formaldehyde (antibacterial)

Sulfonamides (form compounds w/ formaldehyde)
Hippurate
Antibiotic
Urinary Antiseptic (ph <5.5)
Release formaldehyde (antibacterial)

Sulfonamides (form compounds w/ formaldehyde)
Nalidix Acids
Antibiotic
Urinary Antiseptic (pH <5.5)
Coliform UTI
Oxolinic Acids
Antibiotic
Urinary Antiseptic (pH <5.5)
Coliform UTI
Chloramphenicol Resistance
Chloramphenicol acetyl transferase causes resistance
Tigecycline
Antibiotic
Tetracycline
Slow IV, 42.4 hr half-life

Use in vancomycin-resistant

Hepatotoxicity, phototoxicity, bone/teeth devo
Children, pregnancy

Doxycycline
Antibiotic
Tetracycline
16-20 hr half-life

Hepatotoxicity, phototoxicity, bone/teeth devo
Children, pregnancy
Minocycline
Antibiotic
Tetracycline
16-20 hr half-life

Hepatotoxicity, phototoxicity, bone/teeth devo
Children, pregnancy
Tetracycline Resistance
Less 30S affinity
Tolfnaftate
Antifungal
Anti-Dermatophyte
Terbinafine
Antifungal
Anti-Dermatophyte
Nail infections
Block ergosterol synth (buildup of squalenes)

Pregnancy
Griseofulvin
Antifungal
Anti-Dermatophyte
Toenail fungus
Oral (only oral anti-dermatophyte)
Disrupts mitosis
Miconazole
Antifungal
Anti-Dermatophyte; Mucocutaneous
Non-triazole
Topical (yeast infections, athlete's foot)

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Clotrimazole
Antifungal
Anti-Dermatophyte; Mucocutaneous
Non-triazole
Topical, throat

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Fluconazole
Antifungal
Anti-Dermatophyte; Systemic; Mucocutaneous
Triazole (less tox)
Chronic infections

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Itraconazole
Antifungal
Anti-Dermatophyte; Systemic; Mucocutaneous
Triazole (less tox)
Oral & injection

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Ketoconazole
Antifungal
Anti-Dermatophyte
Triazole (less tox)

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Azoles
Inhibit ergosterol synthesis by preventing lanosterol demethylation
Broad spectrum (candidiasis, dermatophytes, aspergillosis)
Need stomach acid to be absorbed!

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Voriconazole
Antifungal
Anti-Dermatophyte; Triazole (less tox)
Most potent!

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Posaconazole
Antifungal
Anti-Dermatophyte; Triazole (less tox)
Aspergillis in immunocompromised

Inhibit P450 & steroid production, hepatotoxicity, GI upset
Flucytosine
Antifungal
Systemic
Fluoridated pyrimidine
Turns into FdUMP & FUTP --> X RNA & DNA synth
NEVER alone b/c of resistance

GI upset, enterocolitis, hepatotoxicity, bone marrow tox/anemia
Flucytosine Resistance
Permease mutation
Sensitive fungi must have permease enzyme
Caspofungin
Antifungal
Systemic
Inhibit beta-glucan synthesis
Used when other antifungals don't work
Micafungin
Antifungal
Systemic
Inhibit beta-glucan synthesis
Used when other antifungals don't work
Amphotericin B
Antifungal
Systemic; Mucocutaneous
Gold standard acute treatment for advanced infx
Polyene; pokes holes in ergosterol of membrane
Oral (GI), IV, catheter (bladder)

Hypersentivity, nephrotoxicity
Nystatin
Antifungal
Mucocutaneous
Polyene; pokes holes in ergosterol of membrane
NEVER systemic (topical)
Acyclovir
Antiviral
No viral DNA polymerase
HSV, varicella zoster
IV (bad oral bioavailability)

GI, nephrotoxicity, headache
Valacyclovir
Antiviral
Acyclovir Analog
HSV, CMV
Famciclovir
Antiviral
Acyclovir Analog
HSV, CMV
Ganciclovir
Antiviral
Acyclovir Analog
CMV
Valganciclovir
Antiviral
Acyclovir Analog
CMV
Foscarnet
Antiviral
Inhibits viral DNA polymerase
HSV w/ HIV, CMV

Less marrow suppression
Gamma-Globulins
Antiviral
Block absorption & penetration of virus
Give during incubation period
Zanamivir
Antiviral
Inhibits neuraminidase; viral cells clump, can't be taken up
Influenza A & B
Amantadine
Antiviral
Reduce uncoating (binds M2, preventing acidity)
Influenza A, Parkinson's
Rimantadine
Antiviral
Reduce uncoating (binds M2, preventing acidity)
Influenza A, Parkinson's
Didanosine
Antiviral
Nucleoside RTI (HIV)

Lactic acidosis, fat wasting, hyperlipidemia
Peripheral neuropathy
Emtricitabine
Antiviral
Nucleoside RTI (HIV)

Lactic acidosis, fat wasting, hyperlipidemia
Abacavir
Antiviral
Nucleoside RTI (HIV)

Lactic acidosis, fat wasting, hyperlipidemia
Tenofovir
Antiviral
Nucleoside RTI (HIV)
Hep B

Lactic acidosis, fat wasting, hyperlipidemia
Zidovudine
Antiviral
Nucleoside RTI (HIV)

Lactic acidosis, fat wasting, hyperlipidemia
Nausea, headache, anemia, neutropenia
Lamivudine
Antiviral
Nucleoside RTI (HIV)
Hep B

Lactic acidosis, fat wasting, hyperlipidemia
Efavirenz
Antiviral
Non-Nucleoside RTI (HIV)
Nevirapine
Antiviral
Non-Nucleoside RTI (HIV)
Indinavir
Antiviral
Protease Inhibitor (HIV)

GI, hyperglycemia, + cholesterol, inhibit P450
Darunavir
Antiviral
Protease Inhibitor (HIV)

GI, hyperglycemia, + cholesterol, inhibit P450
Atazanavir
Antiviral
Protease Inhibitor (HIV)

GI, hyperglycemia, + cholesterol, inhibit P450
Lopinavir-Ritonavir
Antiviral
Protease Inhibitor (HIV)

GI, hyperglycemia, + cholesterol, inhibit P450
HIV Drugs
Combine at least 2 RTIs
Protease inhibitors are standard with 2 RTIs
Enfuvirtide
Antiviral
Fusion Inhibitor (HIV)
Marviroc
Antiviral
Entry Inhibitor (HIV)
Raltegravir
Antiviral
Integrase Inhibitor (HIV)
HPV Vaccine
Antiviral
Preferred for HPV
Trichloroacetic Acid
Antiviral
Topical for genital warts (HPV)
Podophyllin
Antiviral
Topical for genital warts (HPV)
Cryothereapy
Antiviral
Topical for genital warts (HPV)
Sinecatechins
Antiviral
Topical for genital warts (HPV)
Imiquimod
Antiviral
Topical for genital warts (HPV)
Podofilox
Antiviral
Topical for genital warts (HPV)
Simeprevir
Antiviral
Hep C
Telapravir
Antiviral
Hep C
Palivizumab
Antiviral
Hep B & Hep C
Protease inhibitor

Add-on to ribavarin + interferon
Ribavirin
Antiviral
Hep C
Reduces GMP (get less GTP)

Use with interferon
Telbivudine
Antiviral
Hep B
Adefovir
Antiviral
Hep B
Entecavir
Antiviral
Hep B
Interferons
Antiviral
Hep B & Hep C
Activate kinases to inhibit viral protein synthesis
Injection (these are proteins, can't be taken orally)

Flu everyday
Cinacalcet
Calcium Homeostasis
Stimulates Ca receptors, decreases PTH

Uses: hyperparathyroid from chronic renal disease, parathyroid cancer
PTH
Calcium Homeostasis
Rapid effects
Increase plasma Ca, increase bone turnover
Teriparatide
Calcium Homeostasis
PTH analog
Treat osteoporosis
Increase plasma Ca, increase bone turnover
Cholecalciferol
Calcium Homeostasis
Vitamin D3

Uses: rickets, osteomalacia, hypocalcemia, osteoporosis
Vitamin D
Calcium Homeostasis
Slow effects (alters gene expression, protein synthesis)
Calderol
Calcium Homeostasis
Vitamin D


Uses: rickets, osteomalacia, hypocalcemia, osteoporosis

Rocaltrol
Calcium Homeostasis
Vitamin D


Uses: rickets, osteomalacia, hypocalcemia, osteoporosis

Calcipotriene
Calcium Homeostasis
Vitamin D

Uses: rickets, osteomalacia, hypocalcemia, osteoporosis; psoriasis
Doxercalciferol
Calcium Homeostasis

Vitamin D

Uses: rickets, osteomalacia, hypocalcemia, osteoporosis; hyperparathyroid

Calcitonin
Calcium Homeostasis
Made from thyroid
Rapid effects
Decrease plasma calcium, decrease bone resorption

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis

GI upset, hypersensitivity
Calcimar
Calcium Homeostasis
Salmon calcitonin
Decrease plasma calcium, decrease bone resorption

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis

GI upset, hypersentivity
Miacalcin
Calcium Homeostasis
Salmon calcitonin
Decrease plasma calcium, decrease bone resorption

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis

GI upset, hypersentivity
Cibacalcin
Calcium Homeostasis
Human calcitonin
Decrease plasma calcium, decrease bone resorption

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis

GI upset, hypersentivity
Alendronate
Calcium Homeostasis
Bisphosphonate
Decrease bone turnover, bind hydroxyapatite

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis, hyperparathyroid

GI, esophagitis
Ibandronate
Calcium Homeostasis
Bisphosphonate
Decrease bone turnover, bind hydroxyapatite

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis, hyperparathyroid

GI, esophagitis
Zoledronic Acid
Calcium Homeostasis
Bisphosphonate
Decrease bone turnover, bind hydroxyapatite

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis, hyperparathyroid

GI, esophagitis
Risendronate
Calcium Homeostasis
Bisphosphonate
Decrease bone turnover, bind hydroxyapatite

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis, hyperparathyroid

GI, esophagitis
Etidronate
Calcium Homeostasis
Bisphosphonate
Decrease bone turnover, bind hydroxyapatite

Uses: hypercalcemia of neoplasia, Paget's disease, osteoporosis, hyperparathyroid

GI, esophagitis; osteomalacia
Denosumab
Calcium Homeostasis
Decrease RANK-L, decrease bone resorption

Uses: osteoporosis, bone loss from prostate cancer

UTI, respiratory infection, expensive
Prednisone
Calcium Homeostasis; Corticosteroid; Immunosuppression
Decrease Ca absorption from GI, increase renal Ca excretion
Kill T cells
Treat chronic hypercalcemia, inflammation

Chronic --> osteoporosis, aseptic hip necrosis
Fluoride
Calcium Homeostasis
Stabilizes hydroxyapatite, forms fluoroapatite
Increases new bone growth

Fluorosis, nausea, arthritis, CV collapse (extreme)
Estrogens
Calcium Homeostasis
Decrease bone resorption
Treat postmenopausal osteoporosis

Increased breast cancer risk
Raloxifene
Calcium Homeostasis; Estrogen Antagonist
Decrease bone resorption
Treat postmenopausal osteoporosis
Decreases risk of breast cancer

NO increased breast cancer risk
Corticosteroids
From adrenal cortex

Uses: anti-inflammatory, seasonal allergies (Type 1 hypersensitivity), immunosuppression, adrenal insufficiency, adrenal hyperplasia (in utero), topicals (derm & ophtho), leukemia, hypercalcemia, maturation of fetal lungs

New proteins cause effects
Liver metabolism; bile & urine excretion
All ROI

Catabolic, Na/H2O retention, Cushing's, ulcers, cataracts, infections
Hydrocortisone
Corticosteroid
Short-acting
Cortisone
Corticosteroid
Short-acting
Prednisolone
Corticosteroid
Anti-inflammatory
Methylprednisolone
Corticosteroid
Anti-inflammatory
Triamcinolone
Corticosteroid
Anti-inflammatory
Dexamethasone
Corticosteroid; Immunosuppression
Acute anti-inflammatory, for 5-10 days
Kill T cells
Diagnose hypo-pit-adrenal (Cushing's/Addison's means lots of cortisol produced; normal is reduced cortisol)
Betamethasone
Corticosteroid
Acute anti-inflammatory, for 5-10 days
Becomethasone
Corticosteroid
Seasonal allergies
Inhaled
Flunoisolide
Corticosteroid
Seasonal allergies
Inhaled
Aldosterone
Mineralocorticoid
Fludrocortisone
Mineralocorticoid
Mineralocorticoids
Released from zona glomerulosa
Controlled by K+ and RAA system
Spironolactone
Antagonist of mineralocorticoids
Epterenone
Antagonist of mineralocorticoids
Sex Steroids
Released from zona reticularis
Controlled by ACTH
ACTH
From POMC
Testosterone
Sex steroid
DHEA
Weak androgen
Glucocorticoids
From zona fasciculata
Controlled by ACTH
Cortisol is an example
Increase glucose production (usually balanced by insulin)
Cortisol
Glucocorticoid
Made from cholesterol
Pregnenolone = rate-limiting
Need cholesterol esterase & desmolase
Metyrapone
Glucocorticoid antagonist
Stop cortisol
Mitotane
Glucocorticoid antagonist
Stop cortisol
Corticosteroid Release Loop
Hypothalamus -> CRH -> Pituitary -> ACTH -> Adrenal Cortex -> Cortisol -> Effects

Cortisol negatively feeds back on hypothalamus & pituitary
Lispro
Rapid-Acting Insulin
Human
Crystalline Zinc
Rapid-Acting Insulin
IV
Inject 3-4x/day
Aspart
Rapid-Acting Insulin
Glulisine
Rapid-Acting Insulin
Insulin Preparations
Short-acting ones mimic more
Always injected (stays in GI)

Bad with stress, hyperthyroid, stopping exercise, more food, drugs

Hypoglycemia, lipoatrophy
NPH
Intermediate/Long-Acting Insulin
Add with zinc, Lispro, Aspart when need an immediate boost
Detemir
Intermediate/Long-Acting Insulin
2x/day
Glargine
Intermediate/Long-Acting Insulin
No peak, steady insulin
Exenatide
Injectable Hypoglycemic
GLP-1 agonist
Stabilizes beta cells
Delays progress of Type 2

GI, expensive
Pramlintide
Injectable Hypoglycemic
Amylin derivative (normally increases insulin)
Combine with insulin

GI, hypoglycemia
Tolbutamide
1st Gen Oral Hypoglycemic
Most-used
Oral Hypoglycemics
Best for Type 2
Close K+ channels

GI upset, hypoglycemia, less insulin sensitivity
Tolzamide
1st Gen Oral Hypoglycemic
Chlorpropamide
1st Gen Oral Hypoglycemic
60 hr
Metformin
Oral Hypoglycemic
Decreased glucose production
Take with glyburide/glipizide

Metallic taste, lactic acidosis, anorexia
NO hypoglycemia!
Acarbose
Oral Hypoglycemic
Decrease glucose absorbed by meal (inhibits alpha glucosidase)

Flatulence, diarrhea, hypoglycemia
Pioglitazone
Oral Hypoglycemic
Increase insulin-responsive genes
Take with metformin
Repaglinide
Oral Hypoglycemic
Increase insulin secretion
Take with meal
Glyburide
2nd Gen Oral Hypoglycemic
2nd gen's more potent
Gilmepiride
2nd Gen Oral Hypoglycemic
2nd gen's more potent
Glipizide
2nd Gen Oral Hypoglycemic
2nd gen's more potent
Sitagliptan
2nd Gen Oral Hypoglycemic
2nd gen's more potent
Increase GLP-1 & GIP (increases insulin secretion by inhibiting these proteins' metabolism)

GI upset, hypoglycemia
Canagliflozin
2nd Gen Oral Hypoglycemic
For Type 2 only
Releases sugar through the kidney (inhibits sodium glucose transporter; can't reabsorb)

Dehydration, hypoglycemia, UTI
Estradiol
Coagulation, closes epiphyseal plate
Gradually increases during pre-ovulatory stage
Na, H2O retention

Estrogen replacement therapy/contraception
Progesterone
Increases body temp (after ovulation)
Inhibits uterine contraction (stop early labor)
Na, H2O retention

Progesterone replacement therapy/contraception
Danazol
Testosterone
Helps treat endometriosis

Early puberty, prostatic hypertrophy, edema, CNS excitation, hepatotoxicity
Fluoxymesterone
Anabolic Steroid

Early puberty, prostatic hypertrophy, edema, CNS excitation, hepatotoxicity
Nandrolone
Anabolic Steroid

Early puberty, prostatic hypertrophy, edema, CNS excitation, hepatotoxicity
Oxandrolone
Anabolic Steroid

Early puberty, prostatic hypertrophy, edema, CNS excitation, hepatotoxicity
Leuprolide
Antiandrogen
GnRH analog (downregulates GnRH, get less testosterone)
Always with flutamide 1st
Flutamide
Antiandrogen
Androgen receptor blocker
Used for prostate cancer

Low libido, erectile dysfunction
Finasteride
Antiandrogen
Inhibits 5-alpha-DHT
Used for baldness, enlarged prostate
Mifepristone
Progesterone Receptor Antagonist
Treats endometriosis
Abortifation agent (uterine muscle contracts)
Exemestane
Estrogen Inhibitor
Inhibits aromatase (turns androgens into estrogens)
Used in breast cancers
Fulvestrant
Estrogen Inhibitor
Full inhibitor
Trastuzumab
Estrogen Inhibitor
Anti-HER2 antibody
Used in breast cancers
Clomiphene
Estrogen Antagonist
Weak partial ag. at pituitary
Enhances follicular devo
Tamoxifen
Estrogen Antagonist
Estrogen antagonist at breast, agonist elsewhere
Premenopausal
Decreases risk of breast cancer
Conjugated Estrogens
Birth Control
Estrogen-type

Increase breast cancer risk
Decrease endometrial/ovarian cancer risk
Diethylstilbestrol
Birth Control
Estrogen-type
Causes offspring problems

Increase breast cancer risk
Decrease endometrial/ovarian cancer risk
Ethinyl Estradiol + L-Norgestrel
Birth Control
Estrogen-type
Triphasics & biphasics

Increase breast cancer risk
Decrease endometrial/ovarian cancer risk
Mestranol
Birth Control
Estrogen-type

Increase breast cancer risk
Decrease endometrial/ovarian cancer risk
Norethindrone
Birth Control
Progestin-type
Oral

Venous thromboembolism, abnormal uterine bleeding
Etongestrel
Birth Control
Progestin-type
Implant of estrogen

Venous thromboembolism, abnormal uterine bleeding
Levonorgestrel
Birth Control
Progestin-type
Plan B
Localized effects on motility & endometrium

Venous thromboembolism, abnormal uterine bleeding
Hydroxyprogesterone
Birth Control
Progestin-type

Venous thromboembolism, abnormal uterine bleeding
Medroxyprogesterone
Birth Control
Progestin-type

Venous thromboembolism, abnormal uterine bleeding
Progesterone
Birth Control
Progestin-type

Venous thromboembolism, abnormal uterine bleeding
Birth Controls
Venous thromboembolism, abnormal uterine bleeding

Feedback inhibition to hypothalamus. Inhibits FSH & LH
Progestin increases cervical mucus

Lowest dose of estrogen used (increases breast cancer risk)
Pooled Immunoglobulins
Immunostimulation
Treats hypogammaglobulinemia/agammaglobulinemia
INF-alpha
Immunostimulation
Treats cancer, hematologic malignancy
Granulocyte-Macrophage Colony Stimulation Factor
Immunostimulation
Treats myelosuppression
Interleukin-2
Immunostimulation
Activates killer cells
Treats AIDS
Levamisol
Immunostimulation
Antihelminthic
Induces interferons
BCG
Immunostimulation
Viable Mycobacterium bovis/non-viable Corynebacterium parvum
Adjuvants for TB & cancer (stimulates immune system)
Active Immunization
Immunoprotection
Against infections and cancer
Long-lasting
Take advantage of the amplified secondary response
Passive Immunization
Immunoprotection
Against infections
Ig to neutralize antigens
Not long-lasting
Give immediate protection
Epinephrine
Hypersensitivity
Type 1
Theophylline
Hypersensitivity
Type 1
Cromolyn Sodium
Hypersensitivity
Type 1
Inhibits histamine release
Antihistamines
Hypersensitivity
Type 1
2nd generation H1 blockers
Corticosteroids w/ Azathioprine/Methotrexate
Hypersentivity
Type 2
Inhibits autoantibody production
Corticosteroids w/ Azathioprine/Cyclophosphamide
Hypersentivity
Type 3 (immune complex allergies, rheumatoid arthritis, serum sickness)
Combined Immunosuppressives
Hypersensitivity
Type 4 (graft rejection)
Mycophenolate Mofetil
Immunosuppression
Inhibits purine/pyrimidine synthesis
Cyclosporine A
Immunosuppression
Transplants
Inhibit T cell activation & IL-2 formation (inhibition of calcineurin)

Nephrotoxicity, hepatotoxicity, hypertension
Tacrolimus (FK506)
Immunosuppression
Binds FK-binding protein, inhibiting calcineurin --> less IL-2
10-100x more potent than cyclosporine

Nephrotoxicity, neurotoxicity, hyperglycemia
Sirolimus (Rapamycin)
Immunosuppression
Binds FK-binding protein (less IL-2)
Inhibits mTOR (less IL-2 receptors)
Used in a combination for transplants
Antagonizes FK506
Synergizes with cyclosporine A


Increases cholesterol & TGs, GI upset, thrombocytopenia
RhoGam
Immunosuppression
Kills fetal Rh(D)+ RBCs
Prevents Rh hemolytic disease of newborn, immune response of Rh- mother to Rh+ baby
Muromonab
Immunosuppression
Binds CD3 part of T cell receptor
Used for renal rejection AFTER combo therapy failed
Azathioprine
Immunosuppression
Oral
Messes with nucleic acid metabolism, blocks cell-mediated immunity & antibody responses
Combination with prednisone
For severe RA

Leukopenia, rash, fever, hepatotoxicity
Cyclophosphamide
Immunosuppression
Most potent cytotoxic one
Activated by P450
Very large single dose
Kills lymphoid cells

Myelosuppression, cystitis, SIADH (more ADH released; retain water)
Anti-Lymphocyte AB
Immunosuppression
Kills T cells through complement
For transplant & GVHD, pain, anaphylaxis, serum sickness
With azathioprine/prednisone
IM
Adalimumab
Immunosuppression
Anti-TNFalpha
Anakinra
Immunosuppression
IL-1
Etanercept
Immunosuppression
TNF-receptor fusion protein
Infliximab
Immunosuppression
Anti-TNFalpha
Abatacept
Immunosuppression
Anti-CD8
Levothyroxine
Hypothyroid
T4
Choice treatment
Long half-life (1x daily)
Low cost
Not rapid (thyroid hormone regulates gene expression)

Pregnancy - fetal thyroid concentrates it
Liothyronine
Hypothyroid
T3
Short half-life
3-4x more potent than levothyroxine
Higher cost
Not good for routine
Not rapid (thyroid hormone regulates gene expression)

Pregnancy
Thyroid Storm
Fever, increased T3 & T4 levels
From stopping hyperthyroid treatment/too much replacement/131-I

Treat with propanolol (heart rate), PTU & methimazole (less thyroid hormone synthesis), NaI/KI (inhibit thyroid hormone)
Graves' Disease
TSH receptor activating antibodies
Antibody made to thyroidal antigen
131-I
Hyperthyroid
Beta rays
5-day half-life
Destroys thyroid
Treat contamination with NaI (outcompetes)
Iodides
Hyperthyroid
Inhibit hormone release
Decrease size & vascularity of thyroid

Don't take with thiamides/radioactive iodine
Propanolol
Hyperthyroid
Adjunct therapy
Relieves thyroid symptoms
Potassium Perchlorate
Hyperthyroid
Anion inhibitor (inhibits iodide transport)
Blocks thyroidal uptake of iodine

Rarely used - aplastic anemia
Methimazole
Hyperthyroid
Thiazide
Inhibits thyroid peroxidase
Requires depletion of T4

10x more potent than propylthiouracil

Nausea, GI (early); agranulocytosis
Carbimazole
Hyperthyroid
Thiazide
Inhibits thyroid peroxidase
Requires depletion of T4

Nausea, GI (early); agranulocytosis
Propylthiouracil
Hyperthyroid
Thiazide
Inhibits thyroid peroxidase
Requires depletion of T4

Nausea, GI (early); agranulocytosis