QB - PHARM Flashcards
Pentamidine (3)
Pneumocystis jiroveci pneumonia (HIV)
Leishmaniasis
African Sleeping sickness
Nifurtimox
Chagas’ disease (Trypanosoma cruzi)
Mebendazole
Ascariasis
Trichuriasis
Hookworm
Pinworm
Ivermectin
Onchocerciasis (river blindness)
Metronidazole
Giardia lamblia
Entamoeba histolytica
Trichomonas vaginalis
C. difficile pseudomembranous colitis
Giardia lamblia
Metronidazole
Entamoeba histolytica
Metronidazole
Trichomonas vaginalis
Metronidazole
C. difficile pseudomembranous colitis
Metronidazole
Cloroquine, Mefloquine
Plasmodium (malaria)
Primaquine
P. vivax
P. ovale
Methotrexate
Antifolate (cancer therapy)
Trimethoprim
Antifolate (inhibits DHF to THF)
Treats UTI & ear infections
UTI & ear infections
Trimethoprim
Imatinib
CML (bcr-abl tyrosine kinase inhibitor)
Enoxaparin
Low-molecular weight heparin (better bioavailability, longer half-life)
Lepirudin, Bivalirudin
derivatives of Hirudin - INHIBITS thrombin (alternative for heparin)
Clopidogrel, Ticlopidine
Blocks ADP receptors - prevent binding of gpIIb/IIIa to fibrinogen (NO PLATELET aggregation)
For coronary stenting/acute coronary syndrome
Abciximab
Bind DIRECTLY to gpIIb/IIIa on activated platelets - NO PLATELET aggregation
Fibrinogen serves as linker molecule btwn gpIIb/IIIa receptors on two different platelets
Dactinomycin
Doxorubicin
Bleomycin
Intercalates DNA - Antitumor antibiotics
Dactinomycin
Intercalates DNA - antitumor antibiotics
Doxorubicin
Intercalates DNA - Antitumor antibiotics
Bleomycin
Intercalates DNA - Antitumor antibiotics
Cyclophosphamide
Nitrosureas
Alkylating agents - crosslinks DNA
Cyclophosphamide - solid tumors, leukemia, lymphomas
Nitrosureas - brain tumors
Vincristine, Vinblastine
Paclitaxel
Microtubule inhibitors
Vincristine, Vinblastine - block mitotic spindle formation
Paclitaxel - mitotic spindle cannot dissolve (stuck in hyperstabilization) - breast/ovarian cancers
Cisplatin
Crosslinks DNA
Testicular, ovary, bladder cancer; lung carcinomas
Nephrotoxic, acoustic nerve damage
Etoposide
Inhibit topoisomerase II
Hydroxyurea
Inhibit ribonucleotide reductase –> decrease DNA synthesis (S phase)
Rx for CML, sickle cell disease
Prednisone
CLL, non-Hodgkin’s lymphoma
Tamoxifen
SERM - selective estrogen receptor antagonist in breast, agonist in bone
Raloxifene - no increased risk of endometrial cancer (like Tamoxifen)
Trastuzumab (Herceptin)
Breast cancer - cardiotoxic
Rituximab
antibody against CD20
Non-hodgkin’s lymphoma, rheumatoid arthritis
Bevacizumab
Solid tumors
monoclonal antibody against VEGF
Inhibits angiogenesis
Dabigatran, Argatroban
Direct thrombin inhibitors
Prolongs TT (without affecting PT or PTT)
Heparin
Increases antithrombin binding/neutralization of thrombin & factor Xa (prevents clots)
SHORT term management of DVT (deep vein thrombosis)/peri-operative non ambulatory patients
Warfarin
Inhibits Vitamin K dependent clotting factors (II, VII, IX, X)
Inhibits carboxylation of GLUTAMIC ACID residues
Monitor PT/INR
LONG TERM prevention of recurrent venous thrombosis
Lepirudin, Argatroban
Direct thrombin inhibitors
Use for Heparin-induced thrombocytopenia
Ticlopidine, Clopidogrel
Inhibit ADP mediated platelet aggregation
Unstable angina
Rofecoxib
Selective COX2 inhibitor - provides ANTI-INFLAMMATION but does not interfere w/ COX1 (on platelets and in GI tract)
Selective COX2 side effect: increased GI bleeding
Aspirin = irreversible inhibitor of COX1&2
Dapsone, Nitrites effect on blood
Methemoglobinemia (Fe2+ oxidized to Fe3+)
Vincristine
Inhibits microtubule formation (M phase)
Neurotoxic –> peripheral neuropathies
Topoisomerase I and II inhibitors
Hydroxyurea
Inhibits synthesis pathway
Ganciclovir
CMV - MOST COMMON use for HIV patients
Retinitis, esophagitis, pneumonia
polyneuropathy, transverse myelitis, encephalitis
Mechanism of Ganciclovir & adverse rxns
Interferes w/ human host cell DNA synthesis (greater effect than acyclovir)
Adverse rxns:
Neutropenia
Anemia
Thrombocytopenia
What drug used in conjuction w/ Ganciclovir will exacerbate its side effects?
Zidovudine (AZT)
AZT used for HIV patients
Inhibit some mammalian cellular and mitochondrial DNA polymerases –> bone marrow suppression –> anemia, granulocytopenia
AZT + Ganciclovir in HIV patients –> neutropenia & anemia
Ampicillin
Listeria monocytogenes
Meningitis in immunosuppressed
Amphotericin
Cryptococcus neoformans
Meningitis in AIDS patients
Risperidone
Schizophrenia
Side effect: hyperprolactinemia –> amenorrhea
Colchicine
Inhibits tubulin polymerization into microtubules – impairs neutrophil mitosis –> decrease neutrophil motility
Disrupts membrane-dependent functions (chemotaxis and phagocytosis)
Treats GOUTY arthritis
Side effect = abdominal pain, nausea, diarrhea
Avoid using colchicine in what kind of patients?
Elderly w/ renal dysfunction
Terbinafine
Inhibits squalene epoxidase –> NO ergosterol SYNTHESIS
Rx for dermatophytosis
Amphotericin B
Nystatin
BINDS to ergosterol - makes holes in CELL MEMBRANE
Caspofungin
Echinocandin class (INHIBITS CELL WALL synthesis)
Blocks synthesis of B(1,3)-D-glucan
Rx for Candida & Aspergillus
Caspofungin
Flucytosine
Antimetabolite
5-FU in fungal cell - inhibits protein synthesis via RNA miscoding
Cryptococcal infections (given w/ amphotericin B)
Fungal infections
Rx of Endometriosis
Leuprolide
Danazol
Metyrapone
Inhibits production of cortisol
See ACTH surge then product buildup of 11-deoxycortisol (17-OH corticosteroids in urine)
Rx for gouty arthritis
- Indomethacin (NSAID)
- Colchicine (acute relief - inhibits neutrophil migration into inflamed areas)
- Allopurinol (prevention of gout - lowers serum uric acid)
Indomethacin; mechanism? Uses?
Close patent ductus arteriosus (lowers prostaglandins)
COX1 & COX2 inhibitor – suppresses prostaglandin synthesis –> anti-inflammatory agent & pain reliever
Rx for septic arthritis
Ceftriaxone - gonococcus infection
Somatosatin analogs
Octreotide
Lanreotide
Acarbose; what enzyme is inhibited?
Inhibits a-glucosidase
Impairs hydrolysis of sugars (limits postprandial absorption of sugars)
Metformin
Increase sensitivity of target tissue to insulin
Rosiglitazone (a thiazolidinedione)
Similar to metformin (biguanide)
Enalapril
ACE inhibitor - decreases diabetic proteinuria
Glyburide
Sulfonylurea that increases rate of insulin secretion (can see C peptide levels increase as insulin secretion increases)
Colchicine
Acute management of GOUT
Interfere w/ adhesion molecules & microtubule formation responsible for neutrophil chemotaxis and phagocytosis –> reduce inflammation!
Side effect: diarrhea, nausea/vomiting (hence only use colchicine when patients have contraindication to NSAIDs – peptic ulcer/renal failure patients)
Glucocorticosteroids (for gout)
Acute gout - inhibits Phospholipase A2 activity –> less inflammation
What two drugs are contraindicated in acute gouty attacks?
Probenecid
Allopurinol
May exacerbate symptoms
Probenecid
Probenecid - Decrease proximal tubular uric acid reabsorption (decrease uric acid levels)
Rx for gout
Allopurinol
Allopurinol - Inhibition of xanthine oxidase
Rx for gout
Pioglitazone
A type of thiazolidnediones (TZDs)
Binds peroxisome proliferator activated receptor (PPAR-gamma) –> increase ADIPONECTIN synthesis (low levels of adiponectin seen in type II diabetes)
Adiponectin decreases insulin resistance
Side effects: fluid retention, weight gain, precipitation of congestive heart failure
Action of adiponectin
Decreases insulin resistance
Rx for diabetics
Exenatide
Glucagon like polypeptide (GLP-1)
Decrease additional release of glucagon
Increase insulin release
Induce satiety
Decrease gastric emptying (slow rate of sugar absorbed from foods to enter into blood circulation)
DECREASE blood glucose
Major side effects of following drugs:
1. Etanercept
2. Methotrexate or Leflunomide
3. Amiodarone
4. Hydroxychloroquine
5. NSAIDs
- Etanercept: TNF-a inhibitor to treat RA/psoriasis/psoriatic arthritis – need PPD skin test (more susceptible to infectious agents)
- Methotrexate or Leflunomide – Hepatotoxic
- Amiodarone - Pulmonary fibrosis
- Hydroxychloroquine - Ophthalmologic
- NSAIDs - GI blood loss
TNF-alpha inhibitors for RA treatment
Infliximab
Etanercept
Adalimumab
Infliximab
TNF-alpha inhibitors – RA treatment
Etanercept
TNF-alpha inhibitors – RA treatment
Adalimunab
TNF-alpha inhibitors – RA treatment
Inhibitors of purine/pyrimidine synthesis for RA treatment
Methotrexate
Leflunomide
Azathioprine
Methotrexate
Inhibitors of purine/pyrimidine synthesis – RA treatment
Leflunomide
Inhibitors of purine/pyrimidine synthesis – RA treatment
Azathioprine
Inhibitors of purine/pyrimidine synthesis – RA treatment
Chlorthalidone
Thiazide diurectic
Increase Ca2+ resorption in early distal collecting tubule of nephron
Clomiphene
Selective estrogen receptor modulator
PREVENTS negative feedback inhibition on hypothalamus –> increased FSH and LH release (infertility treatment for women who want to ovulate and get pregnant)
Mitotane
Adrenocorticolytic drug – for adrenocortical carcinoma
Spironolactone
Androgen receptor antagonist - inhibits testosterone synthesis
Treats acne & hirsutism
Gynecomastia & testicular atrophy in men
Also a K+ sparing diuretic
Other drugs (other than spironolactone) to treat hirsutism
Flutamide (testosterone receptor antagonist)
Finasteride (5-alpha-reductase inhibitor)
Haloperidol, Fluphenazine
blocks D2 receptors (dopamine) –> strong cholinergic influence (M1 receptor mediated)
EXTRAPYRAMIDAL effects:
acute dystonic reactions (muscle spasms, tongue protrusions/twisting, eyes deviated upwards)
akathisia (inner restlessness, can’t sit still)
parkinsonism
Diphenhydramine, Benztropine
M1 receptor antagonist
re-establish dopaminergic-cholinergic balance
used to treat extrapyramidal effects
Flumazenil
GABA antagonist - counter acute overdoses of Benzodiazepine
Chlorpromazine, Clozapine
H1-histamine receptor
Sedation
Chlorpromazine, Thioridazine
Low potency antipsychotics
Anticholinergic side effects = confusion, dry mouth, urinary retention
Blocks central and peripheral muscarinic cholinergic receptors
Flutamide
Competes w/ testosterone and DHT for receptors on prostate tumors
(prevents androgen-receptor binding on tumors –> tumors shrink in size)
Need to be administered w/ GnRH agonist
Side effect (androgen depletion): hot flashes, gynecomastia, impotence
GnRH agonists
Leuprolide, goserelin, nafarelin, histrelin
binds GnRH receptors in anterior pituitary – inhibit LH and FSH
decreased LH –> decreased Leydig cell stimulation –> diminished testosterone
Ketoconazole
Decrease synthesis of steroid hormones in gonads/adrenals
Anastrozole
Decreased peripheral androgen aromatization - blocks estrogen production selectively
Treatment of postmenopausal women w/ breast cancer (their greatest source of estrogen is conversion of androstenedione in the adrenal glands to estrone in liver, muscle, fat VIA aromatization
Finasteride
Inhibits 5-a-reductase
Decrease conversion of testosterone to DHEA (dihydrotestosterone) - also abbreviated DHT
discordant decrease in DHT
Alpha-glucosidase inhibitors
Acarbose and Miglitol
Decrease disaccharidase activity at intestinal brush border –> less carbohydrate absorption
Side effect: flatulence, bloating, abdominal pain, rash
Sulfonylurea (mechanism)
Membrane ion channels
Insulin (mechanism)
Surface TYROSINE KINASE-coupled receptors
Glucagon-like polypeptide (GLP-1)
Secreted by intestinal L cells (response to food intake)
Induces satiety, decrease gastric emptying, increase insulin release
GLP-1 acts through cell surface receptors coupled to G protein-adenyl cyclase system
E.g. Exenatide (long acting GLP-1) for DIABETES type II
Bisphosphonates
Osteoporosis, Paget’s disease of bone, malignancy-induced hypercalcemia
Structural analogs of pyrophosphate - compoent of hydroxyapatite
“-DRONATE” endings
Alendronate, Risedronate, Ibandronate
Bisphosphonates make hydroxyapatite more INSOLUBLE - also decrease bone resorption by interfering w/ osteoclasts
Patients need to stay upright for at least 30 mins. to prevent reflux; given in fasting state w/ plenty of water
Be mindful of use in RENAL failure patients
OA
Morning stiffness for <30mins (shorter than RA patients)
Bony swelling of DIP and PIP
Use-dependent joint pain in weight bearing joints (alleviated w/ rest)
Tamoxifen
Raloxifene
SERMs: have different effect on estrogen levels in different tissues
Breast - antiestrogenic effect
Bone - partial estrogen agonist (minimizes bone resorption effect - treats osteoporosis in post menopausal women)
**Endometrium - estrogen agonist (increase incidence of endometrial cancers)
Serum: normalizes LDL (somewhat improves lipid profile)
Other concerns: Thromboembolic disease
Amiodarone
Class III anti-arrhythmic
Side effects:
THYROID dysfunction – induces HYPOthyroidism (treat w/ LEVOTHYROXINE)
blue-gray skin discoloration
corneal micro-deposits
drug-related hepatitis
Long term treatment for gouty arthritis (tophaceous gout)
Uricosuric drugs (avoid in renal failure pts):
Probenecid
Sulfinpyrazone
Xanthine oxidase inhibitors:
Allopurinol** (best)
Zileuton
Lipoxygenase inhibitor
Allergic rhinitis & bronchial asthma
Treatment for Gonorrhea vs. Chlamydia
Gonorrhea = Ceftriaxone
Chlamydia = Azithromycin or Doxycycline
Thiazolidinediones (TZDs)
Decrease insulin resistance by acting on PPAR-gamma –> increase adiponectin levels in type II diabetes
PPAR-gamma activation –> increase fat mass secondary to increased differentiation of preadipocytes into mature adipocytes (adiponectin is cytokine secreted by adipocytes)
Side effect: fluid retention, weight gain, CHF due to fluid retention
Rituximab
CD20+ non-Hodgkin’s lymphoma - B cells
Infliximab
binds TNF-alpha (involved in inflammatory response)
TNF is intercellular signaling protein
RA, Crohn’s disease
Certolizumab
TNF-alpha
also for autoimmune diseases
Imatinib
Philadelphia chromosome positive chronic myelogenous leukemia
kit-positive GIST (gastrointestinal stromal tumors)
Vancomycin resistance
D-Ala-D-Ala to D-Ala-D-Lac
Valproate risk
Neural tube defects (inhibit intestinal folic acid absorption)
Dantrolene
Malignant hyperthermia
Breast cancer
Doxorubicin (cardiotoxic)
Acetazolamide
Carbonic anhydrase inhibitor - PROXIMAL TUBULE –> block reabsorption of HCO3- –> increased urinary pH –> metabolic acidosis (since there’s no bicarb around to buffer)
BAD for kid with diabetes who is admited in acidosis state
Indications for Acetazolamide
Diuretic (proximal tubule)
Open-angle and close-angle glaucoma (decrease HCO3- and aqueous humor formation) –> relieve pressure
Side effects of Acetazolamide
Somnolence
Paresthesias
Urine alkalinization*
Macrolides
Cholestatic hepatitis
Quinolones
Tendon rupture
Tetracyclines in kids
Staining of teeth
Benzodiazepines
Short: 24hrs
TRIAZOLAM - short acting (avoid daytime sleepiness) - treats anxiety/insomnia/acute seziures/alcohol withdrawal
LORAZEPAM - intermediate
DIAZEPAM, FLURAZEPAM - long acting (excessive daytime fatigue, impaired judgement)
Phencyclidine (PCP)
NMDAR inhibition
(NMDA is receptor for excitatory neurotransmitter glutamate)
Moderate use - feelings of detachment + distance
Paranoia, hallucinations
Very hostile and aggressive
Heroin
Opiate
Euphoria, constricted pupils, lethargy, clammy skin, nausea
Amphetamine
NE effects
Used for ADHD
Rapid heart rate, high BP, anxiousness, sweating, tremors, dry mouth, hallucinations
Coacine
Inhibits reuptake of dopamine, NE, serotonin
Blurry vision, tremors, twitching, chest pain, irritability, hallucinations/delusions, high BP+HR
Diazepam
CNS depressant
Confusion, mild amnesia, sedation, slurred speech, low BP and HR
Lysergic acid diethylamide (LSD)
Serotonin receptor agonist
Hallucinations –> delusions –> severe paranoia
Marijuana
Contains tetrahydrocannabinol (THC)
Euphoria, short term memory loss, perception distortion
Silliness, red eyes, slowed reflexes, dizziness, impaired coordination
Beta blockers
Used for relieving tachycardia + chest pain in atherosclerotic coronary artery disease patients
(reduce BP and cardiac work, HR)
Noncardioselect agents precipitate asthma symptoms = bad!
B1 - SLOWS heart rate
B2 - bronchoconstriction + wheezing
Reserpine
Inhibits dopamine entry into presynaptic vesicles = chemical sympathectomy
Guanethidine
Inhibit NE release –> LOWER BP and HR
Tricyclic antidepressants
Cocaine
Inhibit NE reuptake –> INCREASE NE concentration at presynaptic neurons –> constant stimulation
Sympathomimetic: Precipitate ANGINA (coronary artery vasoconstriction) + MI
Cocaine causes INCREASED BP, chest pain, agitation, mydriasis, DRAMATIC symmetric pupillary dilation that remains responsive to light, tachycardia
Nasal mucosal atrophy, partial septum destruction = patient uses cocaine
Phenelzine
MAO inhibitor (decreases rate of inactivation of neurotransmitters by monoamine oxidase –> INCREASE concentration of serotonin, NE, dopamine)
dietary restriction: cheese, wine
Sertaline
SSRI (selective serotonine reuptake inhibitor)
Co-administration w/ MAO inhibitor could result in SEROTONIN SYNDROME: restlessness, hyperreflexia, diaphoresis, tremors (excessive serotonin)
Need to wait 2 weeks after MAO inhibitor discontinuation before beginning SSRI - gives body chance to replenish monoamine oxidase stores (monoamine oxidase responsible for breaking down monoamine neurotransmitters)
Desmopressin uses
Vasopressin (ADH) - used for diabetes insipidus
High dose:
increases factor VIII activity in hemophilia A
treats vWF disease
Leuprolide
analog of GnRH
continuous administration - suppresses LH and FSH
initial transient phase of increase in both testosterone & DHT –> stable decrease in testosterone & DHT
prostatic cancer, precocious puberty, endometriosis
Finasteride
Antiandrogen
BPH via inhibition of a-reductase
Ondansetron
Antiemetic
blocks 5-HT3 seroton receptors
Flutamide
Prostate cancer
androgen inhibitor
Octreotide
Somatostatin analog
Controls symptoms of carcinoid syndrome (flushing, wheezing, diarrhea, syncope)
Sodium valproate
Absence & tonic-clonic seizures
Ethosuximide also good for absence seizures (does NOT treat tonic-clonic)
Carbamazepine
Blocks Na channels (less propagation of action potential)
Complex partial seizures
Generalized tonic-clonic seizures
Trigeminal neuralgia
BIPOLAR
side effect:
- AGRANULOCYTOSIS or aplastic anemia (bone marrow suppression)
- Hepatotoxic
- SIADH
Phenytoin
Blocks Na+ channels prolonging rate of recovery (increase refractory period – blocks further action potentials from firing)
Tonic-clonic seizures
STATUS EPILEPTICUS
Side effects: lymphadenopathy, hirsutism, coarsening of facial features, acne, gingival hypertrophy
Lithium toxicity
Nephrogenic diabetes insipidus
Monitor TSH and BUN
Foscarnet
Treats CMV in HIV patients
(Can also use ganciclovir, cidofovir)
Ganciclovir first line treatment for CMV RETINITIS (but side effect = neutropenia) so shouldn’t give to HIV pt. in bone marrow suppression state already (due to Zidovudine)
Side effect:
HYPOcalcemia, HYPOphosphatemia, HYPOmagnesium
Foscarnet wastes Mg2+ –> DECREASE PTH release –> decrease calcium
LOW Ca2+ and Mg2+ –> seizures*
Acyclovir
Treatment for HSV-2
Nucleoside analog - incorporates into viral DNA chain –> terminates DNA synthesis
Nephro + Neurotoxic
Delirium/tremor
Lamivudine toxicity
Nucleoside reverse transcriptase inhibitor (NRTI) for HIV
peripheral neuropathy
lactic acidosis
Indinavir usage & toxicity
Protease inhibitor (HIV)
fat redistribution
hyperglycemia (insulin resistance)
hypertriglyceridemia
Furosemide, Torsemide, Bumetanide
Loop diuretics (ascending loop of Henle)
Na-K-2Cl symporter blocked
Otoxicity
HCTZ, chlorthalidone
Thiazide diuretic (blocks Na-Cl in DCT)
for edema secondary to HF, renal disease, liver disease
Hyperuricemia
Hypercalcemia*
Triamterene, Spironolactone, Amiloride
K+ sparing diuretic (collecting tubule)
Hyperkalemia
Acetazolamide
Carbonic anhydrase inhibitor (PCT)
Metabolic acidosis (blocks reabsorption of NaHCO3)
Mannitol
Osmotic diuretic - descending limb of Henle’s loop & proximal tubule
Hypernatremia
Pulmonary edema
ACE inhibitors
decreases efferent arteriole of kidneys from constriction
decreases GFR
used for HTN, HF, renal failure patients
Atorvastatin
HMG-CoA reductase inhibitor
muscle toxicity
hepatic dysfunction
Metformin (acid-base effect)
Lactic acidosis
Prazosin
selective alpha-1 adrenergic antagonist
Uses:
HTN
Urinary retention (due to BPH)
side effect: HYPOtension (postural hypotension)
Rituximab
anti-CD20
B-cell lymphomas
rheumatoid arthritis
Infliximab
IgG antibody to TNF-alpha
Rheumatoid arthritis
Ankylosing spondylitis
Crohn’s disease
IL-2
Renal cell carcinoma
Melanoma
Imatinib
CML
Philadelphia chromosome
BCR/ABL protein tyrosine kinase
Omalizumab
anti-IgE
asthma
Abciximab
gp IIb/IIIa receptor antagonist
blocks final step of platelet aggregation
administered during angioplasty in patients w/ acute coronary syndrome
Cetuximab
anti-EGFR
non-small cell lung cancer
CRC
pancreatic cancer
squamous cell carcinoma (head and neck)
Bevacizumab
anti-VEGF
metastatic colon/renal carcinoma
non-small cell lung cancer
recurrent glioblastoma multiforme
Muromonab-CD3 (OKT3)
anti-CD3 antibodies
treatment of acute rejection in patients w/ kidney, heart, liver transplants
anti-CD3 antibodies bind to and inhibit T lymphocytes
Amifostine
free radical scavenger
decrease nephrotoxicity when using Cisplatin (platinum containing chemo drug that crosslinks DNA causing acute renal tubular injury)
decrease nephrotoxicity w/ alkylating chemo agents
Leucovorin
Folinic acid
methotrexate (MTX) overdose
Filgrastim
G-CSF analog
stimulate proliferation and differentiation of granulocytes; used to minimize granulocytopenia after myelosuppressive chemo
Dexrazoxane
Iron chelator
prevent anthracycline-induced (doxorubicin) cardiotoxicity (CHF)
Fomepizole
ANTIDOTE for ethanol (rubbing alcohol) or ethylene glycol (antifreeze) poisoning
Raltegravir
HIV integrase inhibitor (HIV can’t integrate into host genome and use host machinery to make more viral mRNA)
Maraviroc
CCR5/CXCR4 antagonist
Ritonavir, Saquinavir
Protease inhibitor (HIV)
Enfuvirtide
Fusion inhibitor (HIV)
prevents viral attachment to cells
Lamivudine, Tenofovir, Efavirenz
RT inhibitor (HIV)
Desmopressin
Release of factor VIII and vWF from endothelial cells
Treats Hemophilia A (bleeding into joints - hemarthrosis)
also ADH analog - treats diabetes insipidus (increase reabsorption of H20 in collecting tubules)
Metoclopramide
Gastro-prokinetic (increase gastric emptying in patients w/ gastroparesis)
Treats nausea and vomiting
Migraine headache
NNRTI
Nevirapine, Efavirenz, Delavirdine
NNRTI:
inhibits RT of HIV - prevent incorporation of DNA copy of viral genome into host DNA
Ropinirole
Non-ergoline dopamine agonist
Restless legs syndrome
D2, D3, D4 dopamine agonist w/ highest affinity for D3
metabolized by P450 CYP1A2
Alprazolam
Short acting BENZO
Moderate to severe anxiety and panic attacks
Anxiety associated w/ depression
Zolpidem
Short acting BENZO
For insomnia, sleeping on overseas plane trip
Hemicholinium
Inhibits uptake of choline - prevents formation of Ach
Vesamicol
Inhibits packaging of Ach into transport vesicles
Botulinum toxin
Blocks release of Ach (flaccid paralysis)
Metyrosine
Blocks conversion of tyrosine to DOPA
Reserpine
Blocks packaging of Dopamine/NE into vesicles
Guanethidine, Bretylium
Blocks release of NE
Cocaine
TCAs
Amphetamine
Blocks reuptake of NE
Amphetamine
Stimulates NE release
Blocks reuptake of NE
Cholinomimetics (direct)
Bethanechol
Carbachol
Pilocarpine
Methacholine
Bethanechol
activates bowel & bladder
postoperative ileus/neurogenic ileus, urinary retention treatment
Carbachol
carbon copy of Ach
glaucoma, relief of intraocular pressure
pupillary contraction
Pilocarpine
Stimulates sweat, tears, saliva
Open and close angle glaucoma
Resistant to acetylcholinesterase (AChE)
Methacholine
challenge test for ASTHMA
stimulates MUSCARINIC receptors in airway
Cholinomimetics (indirect) - ANTIcholinesterase
Neostigmine
Pyridostigmine
Edrophonium
Physostigmine
Donepezil
Neostigmine
Myasthenia gravis
postoperative/neurogenic ileus
urinary retention
Pyridostigmine
Myasthenia gravis (long acting)
does NOT penetrate CNS
Edrophonium
Myasthenia gravis (diagnosis) – SHORT acting
Symptoms improve (proximal weakness - problems getting up from a chair, walking up stairs, eye drooping)
Physostigmine
Treats anticholinergic toxicity (reverse atropine toxicity) - crosses CNS
Donepezil
Alzheimer’s disease
Helps symptoms but does not cure disease
Side effects of ALL cholinomimetics
exacerbation of COPD, asthma, peptic ulcers
Cholinesterase inhibitor poisoning
(too much acetylcholinesterase inhibitors)
organophosphates poisoning (insecticides)
DUMBBELSS
diarrhea
urination
miosis
bronchospasm
bradycardia
excitation of skeletal muscle/CNS
lacrimation
sweating
salivation
Reveral of cholinesterase inhibitor poisoning
ATROPINE + pralidoxime
Reversal of atropine poisoning
(atropine is muscarinic antagonist - decreases actions of Ach)
Physostigmine (cholinesterase inhibitor to INCREASE Ach)
Muscarinic antagonists
Benztropine
Scopolamine
Ipratropium
Oxybutynin
Glycopyrrolate
Atropine
Mydriasis (risk of acute angle closure glaucoma)
Cycloplegia (loss of accomodation)
Benztropine
treats Parkinson’s disease
Scopolamine
Motion sickness
muscarinic cholinergic ANTAGONIST
Ipratropium mechanism & uses
Asthma & COPD
muscarinic cholinergic receptor ANATAGONIST
Blocks action of Ach on muscarinic receptors (Ach released when vagal nerve stimulated –> parasympathetics –> bronchoconstriction)
Ipratropium is beta2 agonist – bronchodilation
Oxybutynin
anticholinergic
decrease urgency (cystitis)
decrease bladder spasms due to antimuscarinic action to smooth muscle cells
Glycopyrrolate
decrease mucus secretion in airway
decrease drooling
decrease gastric secretion (peptic ulcer)
Atropine
muscarinic antagonist
blocks DUMBBeLLS
increase pupil dilation, cycloplegia
decrease secretions
decrease acid secretion
decrease motility
decrease urgency in cystitis
skeletal m. and CNS excitation mediated by nicotinic receptors (not affected by atropine)
Atropine toxicity
increase body temperature (decrease sweating)
dry, flushed skin (peripheral vasodilation bc of no sweating)
cycloplegia (loss of accomodation)
acute angle closure glaucoma (in elderly)
urinary retention (old men w/ BPH)
hyperthermia (infants)
“hot, dry, red, blind, mad”
Sympathomimetics (direct)
Epinephrine
Norepinephrine
Isoproterenol
Dopamine
Dobutamine
Phenylephrine
Albuterol, Salmeterol, Terbutaline
Ritodrine
Epinephrine
alpha 1&2, beta 1&2
anaphylaxis, glaucoma (open)
asthma
hypotension
Norepinephrine
alpha 1&2, beta 1
NO beta 2
hypotension
(but DECREASE renal perfusion - bad!)
Isoproterenol
beta 1&2
torsade de pointes
bradyarrhythmias (but worsens ischemia)
Dopamine
high dose - alpha 1&2
medium dose - beta 1&2
low dose - D1
SHOCK (renal perfusion bc of D1 relaxing renal smooth m.)
Heart failure
Ionotropic & chronotropic
Dobutamine
beta 1 agonist MAINLY
some alpha 1&2 (inotropic & chronotropic)
HEART FAILURE
Phenylephrine
alpha 1&2
Hypotension
Mydriasis
Decongestant
Albuterol
Salmeterol
Terbutaline
beta 2 agonist MAINLY
some beta 1
metaproterenol & albuterol = acute asthma
salmeterol = long term asthma/COPD
terbutaline = prevent premature uterine contractions
Ritodrine
beta 2 agonist
reduce premature uterine contractions
Sympathomimetics (indirect)
Increase catecholamine release or decrease reuptake
Amphetamine
Ephedrine
Cocaine
Amphetamine
release stored catecholamines
narcolepsy
obesity
ADHD
Ephedrine
releases stored catecholamines
nasal decongestant
urinary incontinence
hypotension
Cocaine
catecholamine reuptake inhibitor
vasoconstriction
local anesthesia
*never give beta blockers if cocaine intoxication suspected (unopposed alpha 1 activation –> severe HTN)
Clonidine
alpha-methyldopa
Sympathoplegics
alpha-2 agonist
decrease sympathetic outflow
HTN (good for renal failure pts. bc it doesn’t compromise blood flow to kidneys)
alpha blockers (nonselective)
phenoxybenzamine
phentolamine
phenoxybenzamine (irreversible)
nonselective alpha adrenergic ANTAGONIST
pheochromocytoma
toxicity: orthostatic hypotension, reflex tachycardia
phentolamine (reversible)
treats patients on MAO inhibitors that eat tyramine-containing foods
alpha 1 selective inhibitors
“-osin” (prazosin)
HTN
urinary retention (BPH)
alpha 2 selective inhibtors
mirtazapine (increase outflow of sympathetics)
depression
Beta blockers
“-olol”
A-M are beta1 selective antagonists
N-Z are nonselective beta antagonists
beta 1 selective prefered for patients w/ comorbid PULMONARY disease (beta 2 antagonists causes bronchoconstriction)
Nonselective alpha&beta antagonists
Carvedilol
Labetalol
PARTIAL beta-agonists
Pindolol
Acebutolol
P450 inducers
Modafinil
Barbiturates
St. John’s wort
Phenytoin
Rifampin
Griseofulvin
Carbamazepine
Chronic alcohol use
P450 inhibitors
Quinidine
Ciprofloxacin
Isoniazid
Grapefruit juice
Acute alcohol use
Erythromycin
Indinavir
Cimetidine
Sulfonamides
Ketoconazole
Amiodarone
Macrolides (some)
Gemfibrozil
Sulfa drugs (8)
Probenecid
Furosemide
Acetazolamide
Celecoxib
Thiazides
Sulfonamide antibiotics
Sulfasalazine
Sulfonylureas
sulfa allergies:
Stevens-Johnson
UTI
pruritic rash, urticaria (hives)
hemolytic anemia, thrombocytopenia, agranulocytosis
“-navir”
protease inhibitor
Saquinavir
“-triptan”
5-HT 1B/1D agonist
Sumatriptan
“-ane”
Inhalational general anesthetic
Halothane
“-caine”
Local anesthetic
Lidocaine
“-operidol”
butyrphenone (neuroleptic)
Haloperidol
“-azine”
Phenothiazine (neuroleptic, antiemetic)
Chlorpromazine
“-barbital”
Barbituate
Phenobarbital
“-zolam”
BENZO
Alprazolam
“-azepam”
BENZO
Diazepam
“-etine”
SSRI
Fluoxetine – side effect: sexual dysfunction
“-ipramine”
TCA
Imipramine
“-triptyline”
TCA
Amitriptyline
“-olol”
b-antagonist
Propranolol
“-terol”
b2 agonist
Albuterol
“-zosin”
a1 antagonist
Prazosin
“-oxin”
Cardiac glycoside (inotropic)
Digoxin
“-pril”
Captopril
“-afil”
Erectile dysfunction
Sildenafil
“-tropin”
Pituitary hormone
Somatotropin
“-tidine”
H2 antagnoist
Cimetidine
H1 blockers (1st generation)
Diphenhydramine
Chlorpheniramine
Dimenhydrinate
Allergy
Motion sickness
Sleep aid
Sedation, antimuscarinic, anti-alpha-adrenergic
H1 blockers (2nd generation)
Loratadine
Fexofenadine
Allergy
Decrease CNS entry (less sedative effect)
Albuterol
Relaxes bronchial smooth muscle (B2)
Salmeterol, Formoterol
Long acting B2 agonist (prophylaxis)
Tremor, arrhythmia (side effects)
Be careful using w/ heart disease patients that may be on B-blocker
Theophylline
Inhibits phosphodiesterase – decrease cAMP hydrolysis – bronchodilation
NARROW TI = cardiotoxic & neurotoxic
Metabolized by P450
Blocks adenosine
Beclomethasone
Fluticasone
Corticosteroids - Inhibit synthesis of cytokines
Inactivate NF-kB (TNF-a not made, no other inflammatory agents)
1st line therapy for chronic asthma
Montelukast
Zafirlukast
block leukotriene D4 receptors
for chronic asthma prophylaxis
Zileuton
5-lipoxygenase pathway inhibitor
block conversion of arachidonic aicd to leukotrienes
Omalizumab
monoclonal anti-IgE antibody - inhibits IgE binding to mast cells
used in allergic asthma
Guaifenesin
Thins respiratory secretions (does not suppress reflex)
N-acetylcysteine
mucolytic - can loosen mucus plugs in CF patients
antidote for acetaminophen toxicity
prevents radiocontrast-induced nephropathy in patients w/ renal insufficiency
Bosentan
Treats pulmonary arterial HTN
antagonize endothelin-1 receptors –> decrease pulmonary vascular resistance
Dextromethorphan
Antitussive (antagonize NMDA glutamate receptors)
Codeine analog
Naloxone given for overdose
Pseudoephedrine
Phenylephrine
Sympthomimemtic alpha-agonistic nasal decongestant
Pseudoephedrine also as a stimulant
Open obstructed eustachian tubes
Toxicity - HTN, CNS stimulation/anxiety
Methacholine
Muscarinic receptor agonist
Asthma challenge testing
Amphotericin B
Nystatin
polyene antifungal
BINDS ergosterol –> pore formation and cell lysis
Terbinafine
inhibits squalene-2,3-epoxidase (ultimately decrease ergosterol synthesis)
accumulates in skin & nails
treats dermatophytoses
Griseofulvin
enters fungal cells
binds microtubules –> inhibits microtubules
Caspofungin
Micafungin
block 1,3-beta-D-glucan synthesis (polysaccharide component of fungal CELL WALL)
Flucytosine
inhibits DNA replication and RNA (protein synthesis) in fungal cells
synergistic w/ amphotericin B
** cryptococcal meningitis
Ketoconazole, Fluconazole
INHIBIT SYNTHESIS of ergosterol
P450 inhibitor (increase conc of other drugs in system)
Increase toxicity:
warfarin
cyclosporine
tacrolimus
phenytoin
isoniazid
rifampin
oral hypoglycemics
Cyclosporine
Decrease IL-2 synthesis –> inhibit T cell proliferation
immunosuppressant (transplant pts)
Chloramphenicol
Inhibits bacterial peptidyltransferase (cant transfer aa from A to P site - can’t form peptide bonds)
Streptomycin
Inhibit INITIATION complex formation
Binds and distorts prokaryotic 30S ribosomal subunit
Clindamycin
Erythromycin
Inhibit TRANSLOCATION
Tetracycline
Inhibit aminoacyl-tRNA binding in A site
Isoniazid
+ rifampin
+streptomycin, ethambutol, and/or pyrazinamide
M. tuberculosis treatment
Cromolyn
Nedocromil
Inhibit mast cell DEGRANULATION
prevention/prophylactic treatment
aspirin hypersensitivity/exercise-induced asthma, seasonal allergies
Glucocorticoids (asthma)
Inhibit phospholipase A2 –> inhibit formation of arachidonic acid –> NO prostaglandins (from COX) & leukotrienes (from lipoxygenase)
Isoproterenol
B1 and B2 adrenergic agonist
Increase HR, CO
Decrease peripheral arterial resistance
Bronchodilation in asthmatics
Indicated in asthma, COPD (but not in pt. with MI)
Selective B-blocker (A-M) vs Non-selective B-blocker (N-Z)
Selective (A-M) B-blockers don’t have pulmonary effects: better for pts. with pre-existing PULMONARY issues
Non-selective: B2 blocker causes BRONCHOCONSTRICTION, peripheral VASOSPASM, predispose diabetics to HYPOglycemia
TB treatment
Rifampin (inhibits bacterial DNA-dependent RNA polymerase) - inhibits transcription
- isoniazid + pyrazinamide + ethambutol
and/or streptomycin
Lithium toxicity
Hypothyroidism - measure TSH levels regularly
Nephrogenic diabetes insipidus
Teratogenic (Ebstein’s anomaly)
Valproic acid toxicity
Hepatitis
Teratogenicity
Fluphenazine
Extrapyramidal symptoms (tardive dyskinesia later on)
Clozapine
Atypical antipsychotic
Agranulocytosis
Seizures
Risperidone
Atypical antipsychotic
hyperprolactinemia
Carbamazepine
Agranulocytosis
Treatment for absence seizures
Ethosuximide
Sodium valproate
Anticonvulsant therapy
Diazepam, Lorazepam, Midazolam
Treatment for gneralized tonic-clonic seizures
Phenobarbital
Treatment for complex partial seizures or generalized tonic-clonic seizures
Carbamazepine
Methylphenidate
Indirect-acting sympathomimetic
ADHD disorder
Narcolepsy
Rapid acting insulins
Lispro
Aspart
Glulisine
Action starts in 15 minutes
Peaks at 45-75 minutes
Regular (short) acting insulins
Action starts in 30 mins
Peaks at 2-4 hours
Lasts 5-8 hours
Given SQ
Used to treat DKA (hypotension, tachycardia in young patient w/ diabetes type I)
Intermediate acting insulin
NPH
Starts working in 2 hours
Peaks 4-12 hours
Lasts 18 hours
Long acting insulin
Detemir
Contains fatty acid side chain that binds to albumin = prolonged action
Works within 2 hrs
Peaks 3-9 hrs
Lasts up to 24 hrs
Slow release insulin
Glargine
insulin analog (long duration of action)
Lasts 24hrs
Allopurinol
Rasburicase
Reduce uric acid levels during tumor lysis syndrome
Prevent acute renal failure in pts. undergoing chemo for high grade lymphomas/leukemias
Denosumab
prevents osteoclast activation (prevents bone loss)
prevents RANKL and RANK interaction
Folinic acid (Leucovorin)
Reverse toxicities of MTX (methotrexate) on GI and bone marrow
Amitriptyline
TCA
block muscarinic receptors receptors (anti-cholinergic)
overdose mimics ATROPINE toxicity
Adverse effect of nonselective B-adrenergic blockers
Masked symptoms of hypoglycemia
Bradyarrhythmias
Worsening of Raynaud phenomenon
CNS depression
Treatment to prevent recurrence of HSV-2
Oral daily valacyclovir, acyclovir, famciclovir after incidence
Ethosuximide
Blocks T-type Ca2+ channels in thalamic neurons –> hyperpolarization
Absence seizures
Drug that mimics atropine toxicity
Amitriptyline (+ other TCAs)
Antimuscarinic
fever, cutaenous flushing, dry oral mucosa, dilated poorly reactive pupils, confusion
Prazosin toxicity
a1-adrenergic blocker
treats HTN and urinary retention (due to BPH)
side effect: postural hypotension
Side effect of nonselective B-adrenergic blockers
masked symptoms of hypoglycemia in diabetics
worsening of Raynaud phenomenon
selective alpha-1 blockers (preference for using these)
no alpha2 blockage (alpha-2 suppresses sympathetics)
selective alpha1 blockage causes less tachycardia
Lamivudine
NRTI
Treatment of HIV-1 and HIV-2
Valacyclovir
Acyclovir
Famciclovir
HSV-2
positive Tzanck smear
genital vesicular rash
MTX and 5-FU both inhibit thymidylate formation; what drug can be used to overcome MTX
Leucovorin (N5-formyl-THF) bypasses DHF reductase – overcome MTX
Leucovorin potentiates 5-FU by strengthening thymidylate synthase
MTX: inhibits DHF reductase
5-FU: stabilizes THF & thymidylate syntheatse –> less thymidylate synthetase available for thymidine synthesis
Drug-induced Parkinsonism can be side effect of antipsychotics; treatment of drug induced Parkinsonism?
Anticholinergics (benztropine and trihexylphenidyl) for patients w/ drug-induced Parkinsonism
Levodopa contraindicated - precipitate psychosis
Dopamine agonists (bromocriptine) - used in idiopathic Parkinsonism BUT NOT in drug-induced Parkinsonism (can exacerbate underlying psychosis)
Mechanism of -statin drugs
e.g. Atorvastatin
Statins inhibit HMG CoA reductase –> DECREASE cholesterol synthesis by liver
Body responds by increasin gLDL receptors on hepatocytes to increase LDL uptake from circulation (therefore decreasing LDL circulating in blood)
Side effects of Haloperidol; why can’t you give it to patients w/ drug-induced Parkinsonism?
Haloperidol = first gen. antipsychotic = dopamine-receptor blocker (causes Parkinsonian symptoms)
Extrapyramidal side effects
What drug is used to noramlize prolactin levels and prevent amenorrhea-galactorrhea?
Dopamine agonists (Bromocriptine)
Drugs that decrease VLDV
Fibrates and nicotinic acid therapy
Decrease hepatic production of VLDL –> treatment for primary hypertriglyceridemia (increased VLDL)
Ezetimibe
Decrease intestinal absorption of dietary cholesterol
Biliary excretion of cholesterol increase or decrease in patients on statins?
Biliary excretion of cholesterol DECREASES in pts. on statins due to decreased synthesis of cholesterol in liver
Treatment for generalized anxiety disorder; why does this drug have low abuse potential?
Buspirone - selective agonist of 5HT(1A) receptor
Dependence does not occur
Reduced potential for abused compared to Benzodiazepines
Amphotericin B
Systemic candidiasis
Nystatin
Oral candidiasis
“swish and swallow”
binds to ergosterol in fungal cell membrane –> formation of pores and leakage of ungal cell contents
Griseofulvin
inhibits fungal cell mitosis @ metaphase
indicated for treatment of dermatophytoses
Penicillins
B lactam antibiotics
Inhibit peptidoglycan cross-links in bacterial cell wall
Terbinafine
Accumulates in skin, nails, adipose tissue
treat dermatophytosis (onychomycoses)
Nicotinic acid (Niacin) use; side effects?
Niacin (vitamin B3) treatment of dyslipidemia
- Decrease synthesis of VLDL and hepatic triglycerides
- Decrease conversion of VLDL to LDL
- Increase HDL
Cutaneous symptoms – flushing, warmth, itching
mediated by prostaglandins (pre-treatment w/ ASA helps symptoms)
Skin side effect of Vancomycin
Red man syndrome - histamine release
Serotonin precursor
Tryptophan
Serotonin importance in neuro drugs
Serotonin = mood regulation
Selective serotonin reuptake inhibitors –> increase serotonin levels –> people happier (antidepressant medication)
NAME?
inhibiting enzyme HMG-CoA reductase
upregulation of hepatocyte LDL receptors –> increased uptake of LDL cholesterol from circulation
Bile acid-binding resins mechanism
Cholestyramine
Colestipol
binds bile acid – intereferes w/ hepatic recycling/reabsorption of bile acids
hepatic cholesterol used in order to re-synthesis more bile acids (since there’s no bile acids around) – increased uptake of LDL from circulation to make bile acids
Bile acid-binding resins (side effects)
Constipating & bloating
Malabsorption of vitamin K
Hypertriglyceridemia – do not use w/ patients that already have hypertrigylceridemia!!
Exacerbate diverticulosis (due to constipating side effect)
Gallbladder stones
Niacin (vitamin B3) - relation to GI
Inhibit hepatic VLDL production
Used to increase HDL levels
Drug of choice for alcohol withdrawal
Long-acting benzodiazepines (chlordiazepoxide, diazepam)
Short-acting benzodiazepines (lorazepam, oxazepam) preferrer for advanced liver dysfunction
Mechanism by which drugs given in alcohol withdrawl works?
Give GABA agonists such as barbituates or benzodiazepines (similar effect as alcohol)
alcohol withdrawl symptoms:
patient who has been in hospital and hasn’t had access to alcohol –> CNS excitation (since there’s no alcohol to stimulate GABA receptors) –> tremulousness, insomnia, anxiety, headache, autonomic hyperactivity (variable BP, diaphoresis, tachycardia)
Baclofen
GABA agonist – spastic conditions
Haloperidol (toxicity)
lowers serizure threshold
Phenobarbital
barbituate anticonvulsant - enhances GABA activity
Treatment for active tuberculosis
Rifampin
Ethambutol
Isoniazid
Pyrazinamide
and/or Streptomycin
Rx for atypical mycobacterial infections (e.g. Mycobacterium avium complex)
Macrolide + Rifampin + Ethambutol
Rx for Staph endocarditis
IV nafcillin + aminoglycoside (gentamicin)
Bacterial resistance to rifampin – mechanism?
genetic mutation of bacterial DNA-dependent RNA polymerase
Rifampin needs to be administered as part of multi-drug regimen
P450 inducer (other drugs will be metabolized more rapidly w/ co-administration with rifampin)
Mycobacterial resistance to isoniazid?
Catalase-peroxidase
or
Genetic modification of isoniazid binding site on mycolic acid synthesis enzyme
Resistance to ethambutol
Inhibit synthesis of mycobacterial cell wall via increase production of arabinosyl transferase
Resistance to Pyrazinamide
Lowers the environmental pH to kill M. tuberculosis
Drug has to be converted to active form via pyrazinamidase (bacterial mutate this enzyme)
Mechanism of digoxin on AV conduction
Decrease AV nodal conduction via increased paraympathetic tone (vagus nerve –> decrease rate of AV conduction –> ventricles contract at more normal rate –> adequate fiastolic filling time –> normal cardiac output)
*prevents rapid ventricular response (usually accompanying a. fib) – which leads to poor CO and backup of blood in lungs (heart failure)
Digoxin effect on ventricular contractility
blockade of NA-K-ATPase on cardiac myocytes –> increased itracellular Ca2+ levels in sarcoplasmic reticulum –> maximal crosslinking of actin and myosin –> increased ventricular contractility
Isoniazid can lead to deficiency of which enzyme?
Vitamin B6 (pyridoxine)
Isoniazid chemically similar to B6:
competes w/ B6 to make GABA –> defective product
Peripheral neuropathy
Drug also increases excretion of B6
Need to give supplemental B6 with Isoniazid
Chronic treatment to prevent bronchial asthma
Fluticasone (inhaled glucocorticoid)
Cortiscosteroids = strongest effect on inflammatory compoenent of astham
(steroids usually end in “-sone”)
Action of glucocorticoids on lungs
Not for treat of acute episodes of asthma
inhibit formation of cytokines responsible for asthma
apoptosis of inflammatory cells (macrophages, lymphocytes, eosinophils)
decrease amount of mucus produced by goblet cells
reduce airway hyperresponsiveness by decreasing inflammation
Nifedipine
DHP Ca2+ channel blocker
Treats HTN
Blocks Ca2+ influx into bronchial smooth muscle cells –> bronchodilation
Acyclovir use
Herpes simplex infections
Clarithromycin + other antibiotics
Mycobacterium avium complex
Leukocyte interferon-a
hepatitis B and C
hairy cell leukemia
condyloma acuminatum (HPV)
Kaposi’s sarcoma
Pentamidine
Pneumocystis pneumonia
Sulfonylurea or meglitnide abuse - action on blood sugar
Increase insulin, c-peptide, pro-insulin levels
bind to ATP-dependent K+ channels on pancreatic beta cells –> inhibit hyperpolarizing potassium current –> depolarization –> Ca2+ channels opening –> exocytosis of secretory granules filled w/ mature insulin & c-peptide
Main site of action of nitroglycerin
Venodilator –> large veins
Treats angina by venodilating –> blood collects in venous system –> decrease preload –> decrease ventricular wall stress –> decrease cardiac O2 demand
Vessels in which nifedipine and prazosin works
Nifedipine (Ca2+ channel blocker)
Prazosin (alpha1-adrenergic blocker)
Small arteries and arterioles – primary site of hormonal regulation of systemic blood pressure and primary vascular site of action of vasoactive antihypertensive drugs
Absence of lamellar bodies of type II pneumocytes
Patchy alveolar atelectasis (collapse)
Neonatal respiratory distress syndrome
Methotrexate (MTX) - mechanism & additional drugs given in conjunction w/
Inhibits DHF reductase –> block folinic acid synthesis
Can be given w/ Leflunomide & TNF-a inhibitors for rheumatoid arthritis
Side effects of MTX
Stomatitis (painful mouth ulcers) - supplement w/ folic acid
Hepatotoxicity
Myelosuppression (increased risk for opportunistic infections)
B cell lymphomas
Pulmonary fibrosis
contraindicated in pregnancy
Side effects of Naproxen
GI bleeding
fluid retention
worsening HTN
Minocycline
Treats early mild rheumatoid arthritis
photosensitivity (mild side effect)
Hydroxychloroquine
main use - SLE
can be used for early mild seronegative rheumatoid arthritis
permanent retinal damage (serious adverse)
Corticosteroid chronic use - side effects?
weight gain
hyperglycemia
bone density, skin striae, proximal muscle weakness
used w/ NSAIDs – potentiate risk for GI bleeding
Valproic acid
blocks NMDA receptors - affects K+ current
can also affect Na+ channels and GABA receptors
Similar mechanism of:
Phenytoin
Carbamazepine
Valproic acid
reducing Na+ channels’ abiltiy to recover from inactivation
Phenoxybenzamine (indication); also effect on insulin
long acting alpha-blocker used for pheochromocytoma
blockage of alpha-receptors –> unopposed beta effects –> increase beta2-adrenergic stimulation = increase insulin release
Diphenhydramine
Antihistamine (blocks H1 histamine receptor)
Anticholinergic activity
Propranolol
Non-cardioselective beta blocker
inhibits insulin secretion – increase risk of diabetes mellitus for patients on long term beta blocker use
Drug used to decrease severity of inflammation and decrease extraocular volume in Grave’s opthalmopathy
Prednisone (high dose glucocorticoid)
Rx that inhibits thyroid peroxidase; how?
Methimazole
Propylthiouracil
Responsible for oxidation (organification) of iodide to iodine at apical-colloid interface
Iodine + tyrosine (on thyroglobulin) –> T1, T2, T3 thyroxin
TCA overdose - cause of death?
TCAs inhibit reuptake of NE and serotonin
Inhibit fast Na+ channels –> arrhythmias (phase 0 prolonged, prolonged WRS complex) –> negative inotropy –> decrease contractility, refractory hypotension, peripheral vasodilation –> v. fib
Rx that causes serotonin syndrome; symptoms?
MAO inhibitor + SSRI (or large doses of SSRI)
hyperthermia, autonomic instability, muscle rigidity, myoclonus, diaphoresis
Examples of TCAs
Imipramine
Amitryptyline
Clomipramine
Treatment for TCA overdose
Normal saline
Hypertonic sodium bicarbonate
Mechanism of Warfarin
inhibits vitamin K dependent g-carboxylation of glutamic acid residues of clotting factors II, VII, IX, X
Reversal of warfarin-induced anticoagulation
Fresh frozen plasma (rapid reversal)
vitamin K (re-synthesis of clotting factors)
Reversal of heparin
Protamine (binds to heparin and inactivates it)
Aminocaproic acid
Antifibrinolytic - inhibits fibrinolysis (inhibits plasminogen)
Acylclovir mechanism of action
Guanosine analog
Needs to be activated by viral thymidine kinase (TK)
acyclovir monophosphate –> phosphorylated to active form –> impairs viral DNA polymerase-mediated replication of virus
Rx for HSV-1&HSV2
Related drugs: Famciclovir
Valaciclovir
EBV and CMV do not have same thymidine kinase as HSV - so drug is not as effective
Medroxyprogesterone (Depo Provera)
Progesterone-only contraceptive via IM injection once every 12 weeks
Medroxyprogesterone acetate
Decreases endometrial hyperplasia (decrease risk of endometrial carcinoma)
Good for postmenopausal women on estrogen replacement
Long-acting contraceptive
Side effect: decreased bone mineral density
Raloxifene
Estrogen agonist: bone, cardiovascular, blood lipoproteins
Estrogen antagonist: breast, uterus
Alendronate
Synthetic bisphosphonate (analog of pyrophosphate)
bone resorption inhibitor
Leuprolide
GnRH analog
agonist - pulsatile administration
antagonist - continuous administration
agonist - estrogen levels increase (protect against osteoporosis)
antagonist - estrogen levels decrease (protect against breast cancer in post-menopausal women)
Cholestyramine
Colestipol
Colesevelam
Bile acid-binding resins - binds bile acid in GI tract - interferes w/ enterohepatic circulation
LDL reduced (hepatic cholesterol used up to make new bile acids) –> increased uptake of LDL from circulation (lowering LDL from blood)
side effect: hypertriglyceridemia, VLDL increase
usually given w/ a statin (but at least 4 hrs apart so that bile-acid resin doesn’t interfere w/ absorption of statin)
Gemfibrozil
Fenofibrate
decrease serum triglycerides by reducing hepatic triglyceride production
Fibrates activate PPAR-alpha –> PPAR-alpha activates lipoprotein lipase
decreased VLDL cholesterol (decreases LDL)
decreased TRIGLYCERIDES
increase HDL
Halothane
Sevoflurane
Have bronchodilation properties – preferred in patients w/ asthma (since inhalation anesthetics tend to cause postoperative atelectasis via suppression of muciliary clearance)
Fluorinated anesthetics - effect on cerebral blood flow
Increase cerebral blood flow (via decreased vascular resistance) –> increased intracranial pressure – bad!
Side effects of inhlation anesthetics
Increased cerebral blood flow –> increased ICP
myocardial depression, hypotension
respiratory depression
decreased renal function
Symptoms of opioid withdrawal in an infant born to mom who abuses opioids
Pupillary dilatation
Rhinorrhea, sneezing, nasal stuffiness
Diarrhea
Chills, tremors, jittery movements
Treatment of choice for acute opioid withdrawal in neonate
Tincture of opium or paregoric
Naloxone
Opioid receptor antagonist
Rx for acute opioid intoxication or overdose
DO NOT give to patients w/ opioid withdrawal – can cause seizures
Folic acid (folate)
RBC production
Lowers homocysteine levels
Prevents neural tube defects
Sodium bicarbonate
IV - treatment for acidosis and hyperkalemia
Oral - alkalinizing agent/antacid
Treatment regimen for M. tuberculosis
Isoniazid - mycolic acid synthesis - disturbs cell wall - disturbs ability of mycobacteria to have acid fast reaction on stain
Ethambutol - inhibit mycobacterial cell wall synthesis (no effect on creation of mycolic acid)
Rifampin - halts protein synthesis via inhibition of bacterial DNA dependent RNA polymerase – prevents transcription of DNA into mRNA
Where does acetazolamide work?
Proximal convulated tubule
Carbonic anhydrase inhibitor
Site of action of loop diuretics; what are they?
Thick ascending limb of loop of Henle
Furosemide
Bumetanide
Torsemide
Ethacrynic acid
Site of action of thiazide diuretics; side effect?
Distal convoluted tubule
Exacerbates hypokalemia
What renal drugs has potential to cause hypokalemia?
Loop diuretics (except K+ sparing ones)
What type of neuro/psych drug causes diabetes insipidus?
Lithium – treats bipolar disease
Lithium inhibits action of vasopression (ADH) –> polyuria & polydipsia
Vancomycin resistance: D-ala-D-ala substitution for mutated sequence; what is the sequence?
D-ala-D-lactate
What renal drug should be given to patient w/ HTN and CHF who also has osteoporosis?
Hydrochlorothiazide – increases absorption of Ca2+ (distal convoluted tubule)
Reabsorption also prevents painful renal stones (from hypercalciuria)
Where does Ca2+ reabsorption take place in renal tubules? What drug causes this?
Distal convoluted tubule – Hydrochlorothiazide
Site of action between osmotic diuretics & loop diuretics?
Osmotic diuretic - descending limb of loop of Henle & proximal tubule (mannitol)
Loop diuretic - thick ascending limb of loop of Henle (furosemide)
Furosemide
Loop diuretic – treats HTN and CHF
Increases urinary Ca2+ LOSS –> worsens osteoporosis in post-menopausal women
Spironolactone
Inhibits testosterone (and other steroid hormones)
Used for antiandrogenic action –> treats hirsutism & androgen-dependent malignancies
Acarbose
Oral hypoglycemic agents
Rx for type 2 diabetes mellitus
Substance in sunscreen to block UVB light
Para-aminobenzoic acid (PABA) esters
Protects against UVB (290-320nm wavelength)
What drug is used to diagnose asthma in pt. who presents w/ asthma symptoms but has normal spirometry values?
Methacholine challenge
Methacholine = muscarinic cholinergic agonist –> bronchoconstriction + increased airway secretions
Administration of Methacholine –> decrease FEV1 by more than 20% indicates bronchial asthama
Varenicline
Partial agonist at nicotinic acetylcholine receptors; only releases limited downstream - LESS stimulation of reward pathways (than nicotine)
Helps patients w/ cessation of tobacco (reduces withdrawal cravings; attenuating rewarding effects of nicotine)
Antidepressant that does NOT cause sexual dysfunction; what are side effects?
Bupropion - does not have sexual dysfunction side effect
has stimulatory effect –> treatment for depression w/ associated psychomotor retardation/hypersomnia
treats nicotine dependence
side effect: agitation, insomnia, seizures
Trazodone
highly sedating anti-depressant (helpful for pts. w/ insomnia)
causes priapism
Antimetabolite = folate antagonist
Methotrexate
Antimetbolite - purine analogs
6-MP
Fludarabine (for CLL)
Cladribine (for hairy cell leukemia)
Cladribine
for Hairy Cell Leukemia
Resistant to adenosine deaminase (adenosine functions in purine disposal pathway)
Antimetabolite - pyrimidine analogs
5-FU
Capecitabine
Cytarabine
Gemcitabine
Lomustine
Nitrosurea
DNA alkylation & cross-bridge formation
Requires non-enzymatic hydroxylation
Penetrates CNS
Dacarbazine
Cell-cycle nonspecific methylating agent
Cisplatin
Pt-containing chemotherapeutic agent – forms cytotoxic metabolite in environments w/ low chloride concentration
Mercaptopurine
Converted to active metabolite by HGPRT
Inactivated by xanthine oxidase
What is administered before bronchoscopy to decrease respiratory mucous secretions & promote bronchodilation?
Atropine
Mechanism of atropine
Anti-muscarinic (anti-parasympathetics)
symptoms of toxicity:
flushed skin, hyperthermia (atropine fever)
mydriasis & cycloplegia
bronchodilation
tachycardia
constipation, urinary retention
Mechanism of physostigmine
Anti-acetylcholinesterase –> increases Ach concentrations
Tertiary amine - capable of crossing blood-brain barrier
(contrast w/ neostigmine & edrophonium – quaternary ammonium structure LIMITS CNS penetration)
Used to reverse atropine toxicity
Significance of HMG-CoA reductase; what drugs target this enzyme?
Statins – inhibit HMG-CoA reductase – reduce LDL cholesterol
HMG-CoA reductase converts HMG-CoA to cholesterol
What drugs taken w/ a statin will increase susceptibility to myopathy (muscle pain + increased serum creatine kinase)?
Statins + fibrates (gemfibrozil or fenofibrate)
Statins alone increase risk of myopathy & hepatitis
Simvastatin - highest associated risk of myopathy
Gemfibrozil - increase concentration of statins
Fenofibrate - causes myopathy by itself
Cholestyramine + statin use common; why must they be dosed at least 4hrs apart?
Cholestyramine (bile acid sequestrant) reduces GI absorption of statins
Combination of fibric acid derivatives + bile acid-binding resins increases risk for?
Cholesterol gallstones (increased cholesterol concentration in bile)
First line treatment for hypertriglyceridemia
Fibrates
Mechanism of niacin
Improves hyperlipidemia by decreasing synthesis of hepatic triglycerides & VLDL
Used in conjunction w/ fibrates to lower TGs
First line treatment for hypercholesterolemia
Statins - inhibits HMG-CoA reductase
Use Ezetimibe to inhibit absorption of cholesterol (if pts. need additional help lowering cholesterol)
Why is ACE-I or ARB preferred for diabetics?
Slow progression of diabetic nephropathy (decrease progression to ESRD)
Antihypertensive effect
Doxazosin
Prazosin
Terazosin
alpha-1 blocker
treats HTN and BPH
Pt. w/ pre-existing coronary arter disease + CHF + HTN; what type of cardioselective beta blockers is needed?
Metoprolol
Atenolol
Hydrochlorothiazide (HCTZ) indications
1st line med for essential HTN
pts. w/ osteoporosis (increases Ca2+)
Isolated systolic HTN
What drug combinations can increase likelihood of gallstone formation?
Gemfibrozil & cholestyramine
Cholestyramine: binds bile acid –> dumps it into bile (increases cholesterol content of bile –> gallstone formation); the good thing about binding bile acids is that liver has to use up LDL to make new bile acids, thus LOWERING LDL in circulation (at the expense of increase risk of gallstone formation)
Gemfibrozil - increase cholesterol content of bile (decrease liver synthesis of TGs)
MOA for Ondansetron, Granisetron, Dolasetron
Blocks vagus-mediated naseau/vomiting (vagal terminals w/ 5-HT3 receptors initiate vagus n. activity in medulla oblongata’s “vomit center”)
Blocks serotonin in chemoreceptor trigger zone
Good for preventing chemo-induced vomiting
Mifepristone (RU-486)
Anti-progestin
Anti-glucocorticoid
Used as abortifacient
Danazol
synthetic androgen
treats endometriosis
treats hereditary angioedema
side effects:
hirsutism
masculinization
fluid retention
weight gain
Drug mechanism of statins vs. bile acid-binding resins
Statins: inhibit HMG CoA reductase –> no cholesterol synthesis –> liver increases LDL receptors on surface to uptake LDL (cholesterol source) from circulation –> this lowers cholesterol in blood
Bile acid-binding resins: Inhibits reabsorption of bile acids –> liver has to make new bile acids by consuming liver cholesterol; also takes up LDL from circulation as cholesterol source to make more bile; statins taken together w/ bile acid-binding resins to avoid this effect
Why is it good to give patient that w/ severe pain and severe hematuria Celecoxib?
Celecoxib is an NSAID and selective COX-2 inhibitor
Does NOT have side effects of bleeding & GI ulceration (platelets only express COX-1)
Both traditional NSAIDs as well as selective COX-2 inhibitors can exacerbate what condition?
Fluid retention –> HTN
Where is COX-2 expressed (other than platelets)?
Vascular endothelial cells & vascular smooth muscle cells –> vascular DILATATION
What protacyclin is increased by COX-2?
PGI2 –> anticoagulation and vascular dilatation
Mechanism of ASA
Irreversibly inhibiting platelet aggregation via ACETYLATION of serine residues of platelet COX enzymes
What Rx (mucarinic Ach antagonists) is used to treat obstructive diseases such as asthma and COPD?
Tiotropium
Ipratorpium
Drugs decrease mucus secretion, decrease bronchoconstriction by inhibit muscarinic Ach receptors (parasympathetics)
Serious side effects of statins?
Myopathy (increase serum CK –> muscle pain = rhabdomyolysis)
Hepatitis
Metabolism of statins through what system?
With exception of PRAVASTATIN, all statin drugs metabolized by P-450 system
Nausea, vomiting associated w/ levodopa use; mechanism? How do you avoid these symptoms?
Peripheral conversion of levodopa –> DOPAMINE
Take Carbidopa (dopa-decarboxylase inhibitor) to limit peripheral conversion of levodopa –> decrease nausea and vomiting
Rx for plasmodium species
Chloroquine = Plasmodium in bloodstream
Primaquine = latent P. vivax and P. ovale in liver
Dietary restrictions & drug-drug interactions of monoamine oxidase inhibitors (MAOIs); examples of MAOIs?
Restrictions = cheese, wine
Drug-drug interactions w/ SSRI
Phenelzine
Tranylcypromine
Indication of Phenelzine
Atypical depression/resistant depression
Mood reactivity
Leaden fatigues (arms and legs feel heavy)
Increased sleep and appetite
Rx for auditory hallucinations
Schizoprenia
Rx: Haloperidol, Chlorpromazine
Bimodal distribution in drug metabolism of Isoniazid; why?
Isoinazid metabolized by ACETYLATION
See bimodal distribution (2 peaks) of drug metabolism: correlates w/ SLOW and FAST acetylators; slow acetylators at higher risk of adverse reactions
What drug used for inflammatory disorders of bowel and skin is metabolized via METHYLATION?
6-mercaptopurine
Common Rx used for invasive MRSA infections?
Vancomycin
Daptomycin
Linezolid
Vancomycin: MOA and adverse effects?
Blocks glycopeptide polymerization via binding to D-ala-D-ala
Adverse:
Red man syndrome
Nephrotoxicity
Daptomycin: MOA and adverse effects?
Depolarization of cellular membrane
Adverse:
Myopathy –> CPK elevation
Inactivated by pulmonary surfactant
Linezolid: MOA and adverse effects?
Inhibits bacterial protein synthesis by binding 50S subunit
Adverse:
Thrombocytopenia
Optic neuritis
High risk for serotonin syndrome
What is the effect on K+ levels in blood when patient is using drugs that decrease aldosterone secretion (e.g. ACE inhibitors)?
Less aldosterone secretion –> less Na+ retention
Na+ and K+ always go in opposite ways
Less Na+ retention –> more K+ retention –> hyperkalemia
ACE inhibitors (eg. Lisinopril) decrease amount of aldosterone secreted – predispose to HYPERKALEMIA;
more intense hyperkalemia when ACE inhibitor used w/ K+ sparing diuretics (amiloride, triamterene, spironolactone)
Pts. with renal insufficiency (more hyperkalemia) or pts. taking K+ supplements
Specific beta-1 blockers
(A-M – “olol”)
Decrease contractility & HR
Inhibit renin release –> antihypertension
Indapamide
Thiazide diuretic
Blocks Na+-Cl symporters in distal tubules
Amlodipine
DHP Ca2+ channel blocker
Blocks vascular smooth muscle –> peripheral vasodilation, improved coronary blood flow
DHP causes SIGNIFICANT vasodilatoin –> REFLEX TACHYCARDIA; can also cause peripheral edema
Medications that can cause HYPERKALEMIA
Non-selective B-blockers (N-Z olol) - inhibits beta-2 mediated intracellular K+ uptake
ACE inhibitors
ARBs
K+ sparing diuretics - block epithelial Na+ channel (ENaC) or aldosterone receptor
Cardiac glycosides (digoxin) - inhibits Na+/K+ ATPase pump
NSAIDs - impaired local prostaglandin synthesis –> reduced renin & aldosterone secretion
Didanosine; use & adverse?
HIV RT inhibitor
Adverse rxn: pancreatitis
Injection of a substance causes blanching of vein, induration & pallor of tissues surrounding IV site – what is occuring? What substance is injected? How can this be prevented?
NE infusion –> NE extravasation –> a1 receptor mediated vasoconstriction –> local tissue necrosis
Tissue necrosis can be prevented by local injection of alpha-1 blocking drug (e.g. phentolamine)
Enalapril
ACE inhibitor
CHF
HTN
Diabetic nephropathy
Isoniazid side effects
Hepatocyte damage
Peripheral neuropathy (need to simultaneously administer pyridoxine)
Indication & major toxicity: Statins
High LDL
toxicity:
hepatitis, myopathy
Indication & major toxicity: Niacin
Low HDL
toxicity:
cutaneous vasodilation
HYPERglycemia (acanthosis nigricans)
HYPERuricemia/gout
hepatitis
Indication & major toxicity: Fibric acid derivatives
(Gemfibrozil & fenofibrate)
High TG
toxicity:
gallstones
myopathy (worse when combined w/ statins)
Indication & major toxicity: Bile acid-binding resins (Ezetimibe)
High LDL
toxicity:
GI upset
Hypertriglyceridemia
Malabsorption
Rx for benign prostatic hyperplasia and HTN
alpha-1 blockers
Doxazosin, Prazosin, Terazosin
Common side effect of K+ sparing diuretics
Gynecomastia (more common w/ spironolactone use than eplerenone)
DHP vs. non-DHP Ca2+ channel blocker
DHP Ca2+ channel blocker: selective for vascular smooth muscle – vessels! (eg. Amlodipine)
Non-DHP Ca2+ channel blocker: selective for heart (Verapamil)
Indications for ribavirin
Nucleoside analog - inhibits guanine nucleotides
RSV or Hep C
Oseltamivir
sialic acid analogue inhibitor
influenza A & B neuraminidases
Amantadine
Impairs UNCOATING of influenza A virion after it is endocytosed by host cell
What drug may precipitate opioid withdrawal when used w/ morphine?
Pentazocine (weak opiod narcotic - produces analgesic effects w/ little abuse potential)
Opioid narcotics = selective mu receptor AGONISTS
Rx for sickle cell anemia; mechanism of drug?
Hydroxyurea increases HbF synthesis
Gardos (Ca2+ dependent) K+ channel blockers inhibit efflux of K+ and H2O from cell –> prevents dehydration of RBCs & reduce polymerization of HbS
Disulfiram
Used for recovering alcoholics
Causes acetaldehyde accumulation –> bad side effects everytime someone consumes alcohol
Metronidazole
Trichomonas vaginitis & bacterial vaginosis
Metronidazole + alcohol = acetaldehyde accumulation (bad side effects) b/c metronidazole inhibits alcohol oxidizing enzymes
What drug can cause atrialization of right ventricle?
Lithium –> Ebstein’s anomaly in infants in utero
Apical displacement of tricuspid valve leaflets –> decrease volume of RV (atrialization of RV)
Lithium used to treat bipolar disease
Infant born w/ irritability, diarrhea, vomiting; could be due to withdrawal symptoms of what?
Narcotic use
Side effect of direct vasodilators? What are some examples of direct vasodilators? What drugs are given in combination to decrease side effects?
Hydralazine
Minoxidil
Used for HTN
Significant arterial vasodilation can cause REFLEX sympathetic activation (sodium and fluid retention to bring BP up) –> tachycardia and edema
Give sympatholytics & diuretics to help w/ side effects
Persistent cough & angioedema - side effect of what Rx?
ACE inhibitor