Pharma Flashcards
maintenance dose formula
what unit will MD be in?
and what if certain dosing interval is given?
MD = Cpss x CL / [bioavailability fraction]
MD unit is mg/min
If dosing interval given, can calc. MD based on that
(eg, 2 mg/min x 60 min/hr x 6 hrs for an MD of 2 and an interval of 6 hrs)
Cpss is steady-state plasma conc.
CL is clearance
bioavailability is 1 if IV
half life formula + how many half-lives to reach Cpss
Vd x 0.7 / CL
steady state conc reached in 4-5 half lives
loading dose formula
changes in loading dose based on organ function?
Vd x Cpss / [Bioavailability fraction]
loading dose stays say, but maintenance dose changes in case of renal/liver issue affecting elimination
anastrozole, letrozole, exemestane
MOA, uses
aromatase inhibitor
postmenopausal breast cancer (blocks aromatization of androstenedione in liver, muscle, fat)
flutamide, cyproterone acetate + spironolactone
MOA, uses
androgen receptor antagonists
tx of metastatic prostate cancer
Cytarabine + Gemcitabine
MOA, differences
both pyrimidine analog antimetabolites; incorporated into DNA > strand termination (no effect on folate metab.)
cytarabine is S-phase specific; gemcitabine is NOT + also has ribonucleotide reductase inhibition
(“cyt” has S sound; “gem” is a real gem… works better)
Fludarabine
MOA, indication
deamination-resistant purine nucleotide analog
inhibits DNA polymerase, primase, ligase and ribonucleotide reductase
used for CLL
5-Fluorouracil
MOA, leucovorin effect
pyrimidine analog that inhibits thymidylate synthetase (after conversion to floxuridine monophosphate)
binds thymidylate synthetase in presence of reduced folate > leucovorin actually INCREASES its toxicity
Interleukin-2
MOA and indications as a drug
activation + differentiation of T-cells to help tumor destruction
approved for renal cell carcinoma and melanoma
Abciximab
MOA + indication
anti-GpIIb/IIIa receptor mAb; blocks final step in platelet aggregation (GpIIb/IIIa binds fibrinogen)
used during angioplasty in ACS
Colchicine
MOA, use, sfx
binds TUBULIN and prevents microtubule polymerization (impairs WBC migration + phagocytosis to reduce gout inflammation)
2nd line in gout, for pt with renal failure, PUD, other NSAID contraindications
GI microtubule disruption > diarrhea (less common nausea, vomiting + pain)
Hepatitis 2-3 days after surgery with anesthesia
cause, s/s, histo
Halothane Hepatitis - halothane is hi-risk, fluranes lower, but still some risk; CYP450 metab > intermediates > immune-mediated hepatitis
fever, nausea, jaundice, tender hepatomegaly OR liver atrophy if severe, anorexia, my-/arthralgia, rash
high LFTs and bilirubin, prolonged PT (may have leukocytosis and eosinophilia, probably and HS rxn)
centrilobular hepatic necrosis (like viral hep)
inflammation of portal tracts and parenchyma
Nitrous Oxide
MOA and toxicity
NMDA antagonism
prolonged exposure > inhibits methionine reductase > megaloblastic anemia
Succinylcholine
MOA, toxicity
depolarizing NMJ blocker
hyperkalemia (esp. burn or SC injury pt)
malignant hyperthermia (ANS issues, rigidity, high temp)
First-line for absence seizures
Detailed MOA, SFX, and 2nd line
Ethosuximide
blocks T-type Ca channels > inhibits rhythmic burst discharges in thalamic neurons
sfx are nausea, vomit, fatigue + hyperactivity
valproate is 2nd line
4 drugs assoc. with acute pancreatitis
azathioprine
sulfasalazine
furosemide
valproate
vinca alkaloids
MOA, phase specificity?
vincristine / vinblastine
inhibit microtubule FORMATION by binding beta-tubulin and preventing polymerization of microtubules
specific to M phase of cell cycle (chromosomes can’t align and segregate)
vincristine
side effect
peripheral neuropathy
disruption of neuronal microtubules > disrupts axonal transport
Cell Cycle + its related chemo drugs
each phase
G1 - cells prepare building blocks for DNA synth
G0 - resting phase
S - DNA replication; topoisomerase I + II inhibitors (etoposide, irinotecan, topotecan) and antimetabolites (MTX, 5-FU, etc.)
G2 - DNA checked for errors + corrections made or apoptosis occurs; intercalators + ROS formers work here (bleomycin, doxorubicin, etc.)
M - division; vinca alkaloids + taxanes
Thiazolidinediones
MOA + effects
PPARy agonist
increased: FA uptake
adiponectin (adipokine that increases adipocyte insulin response + stimulates FA oxidation)
insulin sensitivity
decreased: TNF-alpha and leptin (adipokine that acts on hypothalamus to decrease appetite)
Succinylcholine side effects
Malignant Hyperthermia - especially with halothane co-admin; in genetically susceptible patients
Severe hyperkalemia + life-threatening arrhythmia - in patients with burns, myopathies, denervation or crush injuries
(upregulation of nAChR in denervation > great drug effect)
Bradycardia (PSNS stim) -or- tachycardia (SNS stim)
UFH binds both ATIII and thrombin, increasing ATIII inactivation of thrombin AND factor X
LMWH primarily affects inactivation of which factor?
Mostly just factor X
it has the AT-III binding pentasaccharide, but is shorter and doesn’t bind thrombin
inhibitor of ALCOHOL DEHYDROGENASE
inhibitor(s) of ACETALDEHYDE DH
fomepizole (alcohol DH)
disulfiram (acetaldehyde DH)
metronidazole (acetaldehyde DH)
heparin induced thrombocytopenia mechanism + tx
heparin-PLATELET FACTOR 4 complex causes IgG autoantibodies (about 3-5 days after heparin initiation)
Ab then binds Fc receptor on platelets > activation and clot formation > platelet consumption causes -penia
stop heparin and give direct thrombin inhibitors (bivalirudin or ARGATROBAN) or LMW heparinoids (fondaparinux, danaparoid) to control thrombosis
(don’t give warfarin because necrosis risk is high when thrombosis is already present!)
Trastuzumab
MOA, toxicity
anti-EGFR-2 (HER-2) mAb
cardiotoxicity - HER2 plays role in minimizing cardiomyocyte oxidative stress > antagonism causes DECREASED CONTRACTILITY without signs of destruction or fibrosis
usually ASYMPTOMATIC LV EF REDUCTION, but heart failure can occur
not related to cumulative dose and is often reversible with discontinuation (unlike anthracyclines)
Cholestyramine, Colesevelam, Colestipol
MOA, effects on LDL, VLDL, TAGs
bind GI bile acids > hepatic cholesterol diverted to new bile acid synth > increased LDL uptake > lower LDL
hepatic TAG production increases > HIGHER TAGs and VLDL in circ
Common drug class associated with OLIGOHYDRAMNIOS? why?
results in fetus/child?
ACE inhibitors and ARBs
AT-II is important in fetal renal development > renal maldevelopment > reduced diuresis
results in PULMONARY HYPOPLASIA, skeletal defects, impaired cranial vascularization + hypocalvaria
A patient with epilepsy also has osteoporosis
Why?
Some anticonvulsants (phenobarbital, phenytoin, carbamazepine) also INDUCE CYP450
this can result in INCREASED VITAMIN D CATABOLISM and thus impaired calcium homeostasis
Mechanisms of Isoniazid Resistance (2)
when can isoniazid monotherapy be used?
Decreased catalase-peroxidase - mycobacterial enzyme for activation of drug
Modified protein binding site for isoniazid
Pt with positive PPD but a negative chest x-ray + no other evidence of clinical disease
Bupropion
MOA, most significant side effect + pts at higher risk of it
NE and DA reuptake inhibitor for major depression
SEIZURE - especially at high doses, or in patients with epilepsy or EATING DISORDER
Terbinafine
MOA, uses
inhibits squalene epoxidase
common for dermatophytosis; topical or oral; accumulates in skin/appendages
Theophylline
toxicity effects? tx of toxicity?
nausea/vomiting, abd. pain, diarrhea, ARRHYTHMIA or SEIZURE (seizure is main COD)
activated charcoal
beta blockers
BZD / barbiturate for seizures
DOCs for bacterial vaginosis
their MOAs?
Clindamycin - binds 50s ribosomal subunit; bacteriostatic
Metronidazole - damages DNA of facultative anaerobes; bactericidal
DRESS syndrome
when + how? general sx? other organs affected? labs?
Drug Reaction with Eosinophilia and Systemic Symptoms
2-8 wks after exposure to ANTICONVULSANTS (carbamazepine, phenytoin), ALLOPURINOL, SULFONAMIDES and ABX (minocycline, vanco)
drug-induced HERPESVIRUS reactivation with clonal T-cell expansion cross-reacting with drug
FEVER
generalized LAP
FACIAL EDEMA
generalized morbilliform SKIN RASH (may progress to confluent erythema with follicular accentuation)
may have…
hepatomegaly + jaundice
acute interstitial nephritis
cough + dyspnea
labs - EOSINOPHILIA, atypical lymphocytes, high ALAT
Drug-Induced ANCA vasculitis
which drugs? sx?
propylthiouracil, methimazole, hydralazine
generalized sx, arthralgia/-itis, cutaneous vasculitis
Pharma tx for alcoholism
3 drugs, 3 mechanisms
Naltrexone - mu atg; blocks rewarding effects of alcohol + reduces cravings; depot injection available
Disulfiram - acetaldehyde DH inhibitor; aversion tx
Acamprosate - NMDA modulation
Side effects of maternal terbutaline use in newborn
4
B2 agonist > delays preterm labor
increases risk of…
- neonatal intraventricular hemorrhage (vasodilation)
- hypoglycemia (insulin secretion)
- hypocalcemia
- ileus (relaxes GI SM)
Complications of surfactant treatment in premature newborn (4)
- transient hypoxia (diffusion limitation)
- hypotension
- endotracheal tube blockage (obstruction)
- pulmonary hemorrhage
Thiazides
MOA, mechs of Ca reabs. (2), uses for Ca reabs.
blocks Na-Cl cotransporter in DCT
- Less Na-Cl reabs. apically > more Ca-Na exchange basally (Na into cell, Ca into circ.) > more Ca reabs. via apical channel
- Hypovolemia induced by drug > more Na/water abs. in PCT > more paracellular Ca reabs. in PCT
Ca reabs. by thiazides can…
- Improve osteoporosis
- PREVENT CALCIUM STONES
Linezolid
important drug interaction
Linezolid has MAOI activity > interaction with SSRIs, TCAs, other MAOIs can cause serotonin syndrome!
tx with cyproheptadine
(ex: pt with depression history tx for cellulitis; linezolid is good for Gram+)
hydroxyurea
indication, MOA
sickle cell anemia
increases production of HbF via unknown mech
MOA of non-hydroxyurea sickle cell anemia tx
Gardos channel blockers
Ca-dependent K channels regulate K and water flow across RBC membrane > block them and prevent RBC dehydration
Acyclovir
MOA, activation, resistance
guanosine analog for HSV1/2 and VZV
P-ated by viral THYMIDINE KINASE then double P-ated by host kinases > inhibits DNA polymerase
EBV and CMV do not have the same thymidine kinase
Maraviroc blocks what?
Enfuvirtide blocks what?
Maraviroc - CCR5 antagonist; blocks entry
Enfuvirtide - gp41 antagonist; blocks fusion
MOA of systemic progestins in birth control?
examples
suppress GnRH > FSH/LH > inhibit ovulation
Combined hormonal contraceptives (pill, patch, ring)
Progestin implants/injections
MOA of locally-acting progestins in birth control?
examples (2 categories, one with diff MOA)?
Thicken cervical mucus, impair sperm penetrations
Progestin-only pill (norethindrone)
Levonorgestrel IUD
(Copper IUD - cytotoxic inflammatory response in uterus impairs sperm migration)
Clomiphene citrate
what is it? MOA?
selective estrogen receptor modulator
stimulates FSH + LH production
used as a fertility drug, or to help ovulation occur in PCOS
SPECIFIC mechanism of action of NRTIs
not just chain termination / reverse transcriptase inhibition
NRTIs are nucleoside/-tide analogs that LACK A 3’ OH GROUP
this means they can not form a PHOSPHODIESTER BOND with the next nucleotide > chain termination
Tx for Wilson disease
D-penicillamine, trientine (copper chelators)
Zinc (decr. Cu absorption)
Cyanide poisoning
mechanism?
binds FERRIC (3+) iron > inhibition of CYTOCHROME C OXIDASE in mitochondria
disrupts oxidative phosphorylation > severe LACTIC ACIDOSIS and death
Cyanide poisoning
presentation?
labs?
REDDISH SKIN tachypnea HA tachycardia nausea/vom confusion + weakness
progress to seizure + CV collapse
severe LACTIC ACIDOSIS
NARROW AVPO GRADIENT - tissues can’t use O2
Cyanide poisoning
tx? (3 things)
inhaled AMYL NITRATE - makes METHEMOGLOBIN (Fe2+ becomes Fe3+) with high affin. for CN
HYDROXYCOBALAMIN and SODIUM THIOSULFATE create non-toxic metabolites with CN that are excreted in urine
What is Doxepin?
a TCA
Tx for delirium-associated agitation and psychosis in elderly
(Delirium is acute-onset confusion state secondary to infection etc.; more common in elderly or cognitive disorder)
first-gen antipsych (HALOPERIDOL)
some second gen antipsychs
Status epilepticus tx
first + fastest? good for maintenance?
- IV Benzo - lorazepam or diazepam, fast onset
- Phenytoin - slower onset, for maintenance
- Valproate
Mechanism and tx of TCA arrhythmias
FAST SODIUM CHANNEL blockade causes QRS and QT prolongation
SODIUM BICARBONATE tx - increases serum Ph > favors non-ionized, neutral form of the tca > can’t access sodium channels
(also increases EC sodium > overcomes the competitive blockade by tcas)
What are the 3 types of EPS that occur with antipsychotics?
ACUTE DYSTONIA - sudden-onset sustained muscle contraction
AKATHISIA - subjective restlessness; unable to sit still
DRUG-INDUCED PARKINSONISM - tremor, rigidity, bradykinesia
Aside from the 3 EPS (dystonia, akathisia, parkinsonism), and neuroleptic malignant syndrome…
what is the other movement-related side effect of antipsychotics?
when does it present?
TARDIVE DYSKINESIA
involuntary movements such as LIP SMACKING, biting, grimacing, tongue protrusion or CHOREOATHETOID movements (migrating contractions with twisting/writhing movements)
occurs after CHRONIC use of anti-psychs
What is the first (earliest) EPS that might present in a patient on anti-psych drugs?
tx?
in HOURS to DAYS…
ACUTE DYSTONIA may present with acute-onset involuntary contraction of NECK, MOUTH, TONGUE or EYE muscles (esp. with high dose first-gens)
tx with ANTICHOLINERGICS (diphenhydramine, benztropine)
What is a minor EPS that might present later than acute dystonia via anti-psych tx?
tx?
AKATHISIA presents in DAYS to WEEKS after tx start
from mild subjective tension to marked physical restlessness
tx is lower dose, or give BETA BLOCKER or BZD
Caspofungin + other -fungins (echinocandins)
MOA, indications
(resistant fungi)
inhibits GLUCAN synthesis > fungal cell wall inhibition
good for CANDIDA and ASPERGILLUS
(bad for Crypto, limited activity for Mucor/Rhizopus)
OCPs in treatment of PCOS
mechanism
oral contraceptives work by inhibiting GnRH > inhibiting LH secretion > decreasing androgen synthesis
also increased SHBG synth in liver > less free testo
Med for decreasing FACIAL HAIR GROWTH in hirsutism
mechanism?
Eflornithine (topical)
ornithine decarboxylase inhibitor > affects DNA stabilization and repair > decr. cell growth + increased apoptosis
Fibrates
MOA (3)? effects?
- activate PPAR-alpha > induces HDL synth
- increase LPL activity > clears TAGs
(3. decrease VLDL production)
decrease TAGs by 25-50%
increase HDL by 5-20%
new onset htn and elevated creatinine in pt on immunosuppression
likely drug cause? mechanism?
possible reason for new toxicity from this drug?
CALCINEURIN INHIBITOR NEPHROTOXICITY (cyclosporin, tacrolimus)
dose-dependent RENAL VASOCONSTRICTION and TUBULAR CELL DAMAGE > may cause ARF
toxicity may suddenly develop due to CYP inhibition (metab’d by CYP3A; eg, drinking grapefruit juice)
Pharma tx for restless leg syndrome?
behavioral / environmental tx?
deficiency of what seen in RLS? + other causes?
Dopamine agonists - ropinirole, pramipexole
avoid triggering factors - alcohol, sleep deprivation
IRON defic. seen often; also uremia, and diabetic nephropathy
Oseltamivir
MOA?
Neuraminidase inhibition (both flu A and B)
inhibits VIRAL RELEASE from infected cells
also slows viral penetration into mucous of respiratory epithelium
Amantadine for flu
MOA?
impairs UNCOATING or DISASSEMBLY of virion of INFLUENZA A ONLY after endocytosis
via M2 CHANNEL inhibition (H+ ion channel)
Ganciclovir
structure/MOA?
side effects (think of the MOA)
guanine nucleoside analog (competitive inhibition of GTP incorporation by CMV DNA polymerase)
also slightly inhibits human DNA polymerase > hematologic side effects
NEUTROPENIA, ANEMIA + THROMBOCYTOPENIA
Buspirone
mechanism? onset? indication?
advantages?
5HT-1A partial ag
slow onest (up to 2 weeks)
for generalized anxiety disorder
(NOT for panic disorder)
fewer sedative/hypnotic effects than BZDs
no euphoria, tolerance, dependence or withdrawal
common CYP450 inhibitors
9 items on list, a couple of em have 2-3 drugs/classes
Alcohol - acute use Amiodarone Azoles Cimetidine Diltiazem, verapamil Grapefruit juice Isoniazid, macrolides (not azithro!), quinolones Protease inhibitors SSRIs
(AaaahK! DaG! IPS!)
common CYP450 inducers
ABC GoMPeRS
Alcohol - chronic Barbiturates Carbamazepine Griseofulvin Modafinil Phenytoin Rifampin St. John's wort
most use dependent class of antiarrhythmic?
Class IC - propafenone and flecainide
slowest to dissociate, and do so mostly during diastole > bind longer at faster HR
(QRS duration normally reduced during exercise but these will increase it)
which antiarrhythmics show “reverse use dependence”?
consequence?
Class III - K channel blockers
slower heart rate = longer QT interval prolongation
Labetalol
receptors affected?
alpha 1 - competitive, reversible atg
beta 1 - atg
beta 2 - PARTIAL AG
Praziquantel
MOA, indications
increased Ca++ perm > paralysis, dislodgement + death
cestodes (tapeworms) and trematodes (flukes)
(incl. schistosomiasis, clonorchis, cysticercosis etc.)
Bithionol
moa, indication
inhibits adenylyl cyclase
fasciola hepatica (liver fluke)
Diethylcarbamazine
MOA, indication
inhibits arachidonic acid metabolism in filariae
lymphatic filariasis (elephantiasis)
Wuchereria bancrofti infection (pulmonary eosinophilia)
Loa loa infection
Niclosamide
MOA, indication
inhibits glucose uptake and both aerobic + anaerobic metabolism by worms
TAPEWORMS:
diphyllobothrium latum
taenia spp.
hymenolepis nana (dwarf tapeworm)
-bendazole anthelmintics
MOA, indications
binds B-tubulin > inhibits microtubule polymerization
cell motility and metabolism disruption
flatworms (trematodes)
roundworms (nematodes)
incl. trichuriasis (whipworm), enterobius (pinworms), echinococcus (hydatid disease), neurocysticercosis (T solium) and ascariasis
3 drugs used to lower portal hypertension in acute variceal hemorrhage pts
2 are use more, 1 has limited use due to unwanted effects
- SOMATOSTATIN - inhibit release of endogenous hormones (glucagon, VIP, etc.) that induce splanchnic vasodilation; less splanchnic blood flow > less portal blood flow
- OCTREOTIDE - sst analog; longer acting
- VASOPRESSIN - induces splanchnic vasoconstriction… but also systemic vasoconstriction
What is Pentagastrin and why is it used?
synthetic gastrin analog - used diagnostically
induces CALCITONIN secretion from MEDULLARY THYROID CANCER and…
SEROTONIN release from CARCINOID tumors
Main pharma tx for pulmonary arterial hypertension?
MOA
BOSENTAN
an endothelin receptor antagonist
decreases pulmonary arterial pressure and lessens progression of vascular remodeling + RV hypertrophy
(but lung transplant is the definitive tx for PAH)
pharma tx for anorexia nervosa if CBT and nutritional rehab don’t work
Olanzapine
pharma tx for bulimia nervosa
SSRI
in combo with CBT and nutritional rehab
pharma tx for binge eating disorder (2)
SSRI, or…
Lisdexamfetamine
Suffix of protease inhibitors for HIV
examples
-navir
indinavir, ritonavir, darunavir, atazanavir, lopinavir
3 main sfx of HIV protease inhibitors
- Lipodystrophy - buffalo hump
- Hyperglycemia - increased insulin resistance; may cause DM
- CYP inhibition
Main important drug interaction of HIV protease inhibitors + the solution to it
(not just CYP inhibition, but a specific drug-drug interaction)
If HIV pt has TB…
Rifampin will INDUCE CYP450 and DECREASE SERUM LEVELS of protease inhibitors
Rifabutin can be used instead, and will not induce CYP450
Side effects of fluranes by system
CV? Resp (one positive sfx)? CNS? Kidney? Liver?
- CV - myocardial depression > low CO, high atrial + ventricular pressures, hypotension
- Resp - low Vt and minute V > hypercapnia; impair mucociliary clearance > post-op atelectasis; BRONCHODILATION by halothane/sevoflurane good for asthmatics
- CNS - increase cerebral blood flow > INCREASE ICP
- Kidney - lower GFR, RPF; increase resistance
- Liver - decrease blood flow; HALOTHANE HEPATITIS
drug used for depressive phase and maintenance phase of bipolar treatment
lamotrigine
drugs used for acute mania tx and maintenance of bipolar (3)
carbamazepine
valproate
lithium - not great for acute, takes time
Which diuretics IMPROVE SURVIVAL in patients with HF with lowered EF?
Mineralocorticoid antagonists - SPIRONOLACTONE and EPLERENONE
decrease remodeling and myocardial fibrosis
Contraindication for SGLT2 inhibitors
test what before prescribing?
moderate to severe kidney failure
test creatinine and BUN
Anti-retroviral drug with an adverse reaction connected to a certain HLA haplotype
what’s the drug? what’s the haplotype?
ABACAVIR - an nrti
HLA-B*57:01
(negative test for this allele has near 100% NPV)
Anti-retroviral drug with an adverse reaction connected to a certain HLA haplotype
what’s the drug + what’s the reaction?
ABACAVIR hypersensitivity reaction
abacavir binds directly to HLAB*57:01 > alters presentation of self-peptides > TYPE 4 HYPERSENSITIVITY
fever, malaise, GI sx and DELAYED RASH
two 2nd gen anti-psychs with worst risk for metabolic syndrome?
olanzapine
clozapine
(test BMI, abd. circumference, glucose, lipids, and BP)
Nitrate mechanism for angina relief
VENODILATION > increased venous capacitance
decreases preload and LVEDP > reduces systolic wall stress and O2 demand + increases myocardial perfusion
Dopamine antagonists are best used for what kind of nausea / emesis?
“central nausea” as seen in migraines (they also reduce migraine pain)
also any nausea caused by emetogenic substances affecting the AREA POSTREMA (“chemoreceptor trigger zone”) in the medulla
5-HT3 atgs are best used for what kind of nausea / emesis?
mechanical or chemical irritants in the GI tract
as sensed by the glossopharyngeal and vagus nerves
What is the PG analog used to treat glaucoma?
MOA? Sfx?
Lanaprost
prodrug converted by esterases in cornea > INCREASE OUTFLOW in the uveoscleral pathway by decreasing collagen content
increase pigment in eyelashes and iris
What is the mechanism by which carbonic anhydrase inhibitors treat glaucoma?
inhibit BICARBONATE formation in ciliary body > decrease Na and fluid transport
What two adrenergic actions affect aqueous humor production? Drug names?
Brimonidine - alpha1 > ciliary body vasoconstriction
Timolol - beta2 > decreased production
Milrinone
MOA? Effects?
Indications? Contra?
Selective PDE3 inhibitor
- decrease cAMP degradation > cAMP promotes Ca++ influx > increased contractility
- also inhibits SM PDE > vasodilation
- Refractory heart failure with LV systolic dysfunction
- CI in hypotension
HIV drugs that can cause myopathy?
integrase inhibitors
raltegravir, dolutegravir
GI side effect of opiates other than constipation and nausea
BILIARY COLIC
mu agonists can cause contraction of SM in sphincter of Oddi > increased common bile duct pressure
severe pain + cramping in RUQ
(discontinue drug and give NSAIDs)
Aside from ophthalmological exams…
what eye-related indication does ATROPINE have? (2 names)
IRIDOCYCLITIS aka UVEITIS
reduces pain and prevents adhesions
Tx for beta blocker overdose with hypotension?
Mechanism?
Glucagon
Gs on cardiac myocytes > increased cAMP > increased IC Ca++ release + contractility
Metyrapone MOA
11-beta-hydroxylase inhibitor
blocks cortisol synthesis
what is the MOA/use of filgrastim?
recombinant G-CSF
increases neutrophil count
what is darbepoietin?
EPO with longer half life
blood-gas partition coefficient
what is it? how does it relate to induction rate?
the ratio of an inhaled anesthetic that is DISSOLVED in blood (and thus can bind plasma proteins + stay in blood) to the amount that is UNDISSOLVED/GAS (and thus can diffuse into the CNS)
a high BGPC = higher solubility = slower induction (halothanes + isoflurane)
a low BGPC = lower solubility = faster induction (sevoflurane > N2O > desflurane)
taxanes - paclitaxel and docetaxel
MOA
inhibit microtubule DISASSEMBLY - chromosomes can not segregate
Niacin MOA in hyperlipidemias (2)
- Inhibits HORMONE SENSITIVE LIPASE in adipose tissue
2. Reduces hepatic VLDL synthesis + secretion
PCSK9 inhibitor names
plus sfx
Alirocumab and evolocumab
(Al and Ross Evolved to have less LDL)
Myalgia, delirium + other neurocognitive sx
(main decr. is LDL, slight HDL rise and TG drop)
Drug indicated for both HIV and Hep B?
Lamivudine
aka 3TC … a cytidine analog NRTI
which 4 drugs can cause Fanconi syndrome?
- cisplatin
- ifosfamide
- EXPIRED tetracyclines
- tenofovir
these drugs CITT in the tubules n fuck em up
Other than PTU and beta blockers, what blocks 5’ deiodinase?
glucocorticoids
What should be measured to assess efficacy of EPO tx?
Plasma Hb concentration
(O2 saturation doesn’t necessarily change in anemia, because the Hb that is there is still saturated well; sat mainly changes in CO poisoning, which displaces O2 from Hb)
how do fibrates increase risk of myopathy with statins?
via CYP inhibition
Macrolides MOA - bind what and do what?
bind 50s and interfere with translocation
Drugs causing gout (5)
“Painful Tophi and Feet Need Care”
Pyrazinamide Thiazides Furosemide Niacin Cyclosporine
OTC cough suppressant with possible constipation as a side effect
Dextromethorphan - NMDA atg with some opiate receptor effects
can give naloxone for OD; can cause serotonin syndrome in combo with other drugs
What are the SELECTIVE ARTERIOLAR VASODILATORS (2) ?
what side effects do they have BASED ON PHYSIOLOGICAL COMPENSATORY MECHANISMS that counteract their action?
how does this affect their usefulness?
hydralazine + minoxidil
vasodilation > reflex sympathetic activation > TACHYCARDIA
raas activation > sodium and fluid retention with PERIPHERAL EDEMA
they are not useful long-term due to these compensatory side effects
Hydralazine MOA and indications (3)
increases cGMP > arteriolar vasodilation (decr. afterload)
- SEVERE htn - used acutely
- heart failure - with an organic nitrate
- Htn in pregnancy
Hydralazine
sfx (with 1 related contraindication + 1 sfx treatment)
- Reflex TACHY - CI in angina/CAD; co-admin w BB
- Fluid retention
- HA
- Angina
- LUPUS-LIKE SYNDROME (anti-histone Abs)
Mefloquine
kills what form of plasmodium?
inactive against what + clinical consequence of this?
a SCHIZONTICIDE that kills REPLICATING parasites WITHIN RBCs
is INACTIVATED IN LIVER so does not kill liver schizonts > they rupture over 8-30 days so mefloquine must be taken 4 WEEKS AFTER RETURN FROM ENDEMIC AREA
Which malarial spp. are usually chloroquine resistant?
P. falciparum in Africa
Delirium tremens tx
BZD
specifically LONG-ACTING with active metabolites such as DIAZEPAM or CHLORDIAZEPOXIDE because they self-taper
BZDs for pts with liver disease
acronym
these BZDs do not undergo oxidative metab. in liver
the “LOT” bzds
Lorazepam
Oxazepam
Temazepam
What illicit drug is assoc. with NYSTAGMUS?
PCP - phencyclidine
an NMDA atg
6 medication classes that can cause hyperkalemia
- K-sparing Ds - amiloride, triamterene, eplerenone
- ACE-I - decrease aldo
- Non-selective BB - inhibit B2-mediated K uptake
- ARB - decrease aldo via AT1 atg
- Digoxin - inhibit ATPase
- NSAIDs - decr. local PGs > decreases renin/aldo secretion
KANADN
two NON-SELECTIVE and IRREVERSIBLE mao inhibitors
phenelzine
tranylcypromine
(“try a sip” and “funnel” hooks from sketchy)
(also isocarboxazid … “boxed wine”)
a REVERSIBLE MAO-A inhibitor
Moclobemide
for tx resistant depression / anxiety
2 short-acting (< 6 hour) BZDs
Triazolam
Midazolam
(“try me” i dont last long)
4 medium-acting (6-50 hr) BZDs
Lorazepam
Oxazepam
Clonazepam
Alprazolam
(for when yr feelin a bit “LOCA”)
3 long-acting (>50 hr) BZDs
DIAzepam
Flurazepam
ChlorDIAzepoxide
(lasts todo el “Dia”)
Significant risk associated with Tamoxifen
Endometrial hyperplasia > endometrial cancer risk
blocks breast ERs but is an agonist on endometrial ER
Drugs that can cause AGRANULOCYTOSIS
6, with mnemonic
Can Cause Pretty Major Collapse of Granulocytes
- Carbamazepine
- Clozapine
- Propylthiouracil
- Methimazole
- Colchicine
- Ganciclovir
Drugs that can cause APLASTIC ANEMIA
(6, with mnemonic)
(causes PANcytopenia as opposed to “aplastic crisis” which is RBCs only via impaired reticulocytes by parvo B19 etc.)
Can’t Make New Blood Cells Properly
- Carbamazepine
- Methimazole
- NSAIDs
- Benzene
- CHLORAMPHENICOL
- Propylthiouracil
(note carbamazepine, PTU and methimazole can cause both aplastic anemia + granulocytosis)
What 3 categories of abx bind the 30s ribosomal subunit?
- Aminoglycosides
- Tetracyclines
- Glycylcyclines - tigecycline
1 adverse effect and MAJOR neuro complication possible
Suffix for thrombolytics
“-plase” as in alteplase or tenecteplase - plasminogen activators
HEMORRHAGE is #1 sfx and intracerebral hemorrhage (decr. consciousness, asymmetric pupils, irregular breathing) is main neuro complication
What organisms are resistant to cephalosporins? 5
Altered PBPs - Listeria, Enterococcus, MRSA
No cell wall - Chlamydia and Mycoplasma
