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206 Cards in this Set

  • Front
  • Back
describe bronchial asthma
respiratory syndrome, decreased airflow, inflam of bronchial walls, narrowing airways, increased resistance to airflow; cough, chest tightness, short breath, wheeze
what factors increase airway obstruction
bronchoconstriction (contraction of bronchial smooth muscles), mucosal edema (from inflam), bronchiolar secretions (increased due to inflam)
what drugs can precipitate asthma
B bockers, aspirin, NSAIDS
two kinds of anti-asthma agents
bronchodilators, anti-inflammatory drugs
different kinds of bronchodilators
sypathomimetics (B2 adrenoreceptor agonists, A adrenoreceptor agonists), anticholinergics, xanthines
mechanism and advantages of B2 adrenoreceptor agonists
increase B2 adrenergic receptors on bronchial smooth muscles to get bronchodilation, decrease mediators release from mast cells; most effective, minimal side effects
names of B2 adrenoreceptor agonists
short acting: salbutamol, terbutaline; long acting: salmeterol, formoterol
for B2 adrenoreceptor agonists what is are the indications and route, and maintenance therapy
acute attacks - inhalation, IV infusion; maintenance = oral, inhalation
mechanism, indication and route for anticholinergics and one example
decrease muscarinic receptors, block cholinergically mediated bronchoconstriction; usually adjunct therapy, acute attacks, maintenance; inhalation; ipratropium bromide
3 kinds of xanthines
caffeine, theophylline, theobromide
mechanism of theophylline
decrease phosphodiesterases, decrease cAMP hydrolysis, accumulation of cAMP, relaxation of bronchial smooth muscles, bronchodilation
disadvantages, side effects, and routes for theophylline
narrow therapeutic range, wide range of side effects; CVS - palpitation, dysrhythmias, CNS - tremors, convulsions, GIT - abdominal pain, nausea; oral, IV
4 anti-inflammatory agents (classes of drugs)
glucocorticoids (steroids), mast cell stabilizers, leukotriene receptor antagonists, methotrexate
mechanism and routes of glucocorticoids
anti-inflam effect on bronchial mucosa, decrease macrophages, eosinophils, lymphocytes, decrease mucous secretion; inhale, oral, IV
mechanism, indication, route, example of mast cell stabilizers
stabilize mast cells, decrease release of chemical mediators that cause bronchoconstriction, decrease incidence of asthma attacks; prophylaxis; inhalation; cromolyn sodium and nedocromil
mechanism, indication, route, example of leukotriene receptor antagonists
selective blocking of leukotrienes action on respiratory tract, decrease mucous secretion and bronchoconstriction; adjunct therapy, prophylaxis; oral; montelukast, zafirlukast
indications and side effects of methotrexate
mainly for treatment of malignancies and autoimmune diseases, may reduce requirement of corticosteroids; liver toxicity, bone marrow failure
what is hemostasis
process that retains blood within the vascular system
what is thrombosis
formation of a blood clot (thrombus) within a blood vessel
when does hemostasis occur and what 4 events take place
injury of a blood vessel - loss of vascular integrity; vasoconstriction, platelet activation, blood coagulation and clot formation, fibrinolysis
what does vasoconstriction do
decrease blood flow to injured vessel, decrease blood loss
what happens during platelet activation
platelets adhere to collagen fibrils on injured vessel with help from vWF, platelets aggregate under effect of thrombin and fibrinogen to make a plug, release chemical mediators to activate more platelets
what happens during blood coagulation and clot formation
activation of coagulation factors, coagulation pathway, plug becomes more stable blood clot (fibrin network + blood cells)
what is fibrinolysis, describe
enzymatic process that dissolves fibrin clot, occurs after coagulation, controls size and spread of clot, carried out by plasmin
what are natural anticoagulants, describe
antithrombin - serine protease inhibitor, activated by heparin, inactivates thrombine and factor Xa; protein C - vit K dependent protein, activated by thrombin, inactivates factors V and VIII
what are two kinds of abnormal hemostasis
bleeding disorders, thromboembolic disease
3 bleeding disorders, describe
vascular defects - vasculaitis, purpura; platelet defects - thrombocytopenia, purpura; coagulation factor defects - hemophilias
describe hemophilias, hint: abc, 3 types (what factor is deficient?)
bleeding disorder, congenital or acquired, coagulation factor deficiency, bleeding after trauma or spontaneously; A - factor VIII, B - IX, C - XI
describe thromboembolic disease, examples, tx
group of diseases due to hypercoagulable states; DVT, pulmonary embolism, coronary artery disease; antithrombotic agents as tx
3 types of antithrombotic agents
antiplatelets, anticoagulants (inhibit coagulation factors), thrombolytic (profibronolytic) agents - break down fibrin, fresh thrombus only - acute events
6 antiplatelet agents
cylcooxygenase inhibitors, ADP receptor blockers, phosphodiesterase inhibitors, prostacyclin analogues, adenosine reuptake inhibitors, glycoprotein receptor blockers
mechanism and examples of cyclooxygenase inhibitors
decrease cyclooxygenase enzyme, decrease thromboxane A2; acetylsalicylic acid (aspirin), other NSAIDS (ibuprofen)
describe aspirin, dose, side effects
most powerful platelet inhibitor, more prolonged effect; 350mg/day for myocardial infarction tx, 75-81mg/day for protection; bleeding, peptic ulcer, bronchial asthma
describe ADP receptor blockers, side effects, examples
block ADP receptor, decrease ADP induced platelet aggregation, safe when can't use aspirin; neutropenia, thrombotic thrombocytopenic purpura, bleeding; thienopyridines (ticlopidine, clopidogrel)
describe phosphodiesterase inhibitors, example, indications
selective decrease of PDE3, increase cAMP in platelets, increase active PKA, decrease platelet aggregation; cilostazol; intermittent claudication in peripheral vascular disease
describe prostacyclin analogues, examples
synthetic analogues of prostacyclin, directly increase cAMP levels in platelets; iloprost, carbacyclin
describe adenosine reuptake inhibitors, example
inhibit uptake of adenosine by rbcs, adenosine increases platelet cAMP synthesis, cAMP inhibits platelet aggregation; dipyridamole
describe glycoprotein IIb/IIIa receptor blockers, route, side effects, ex
block receptors on platelets, decrease platelet aggregation; IV; thrombocytopenia; abciximab
two kinds of anticoagulants, subtypes
heparin - unfractioned heparin, LMWH; oral anticoagulants - warfarin, dicoumarol
mechanism, side effects, routes of unfractioned heparin
augments the effects of AT - inhibition of thrombin and factor Xa; bleeding, thrombocytopenia, allergic rx, osteoporosis; IV, SC
difference b/t unfractioned and LMWH, examples
lmw, more selective inhibition of Xa w/ relative sparing of thrombin, less side effects, improved pharmacokinetics, no need for coagulation monitoring, SC injection mainly; tinzaparin, enoxaparin
mechanism of warfarin
vit K is required to activate factors II, VII, IX, X in liver, reduced first by enzyme, warfarin inhibits enzyme
onset, duration, antidote for heparin and warfarin
hep - immediate, short acting (hrs), protamine; warfarin - 2+ days, long (days), vit K
describe thrombolytic agents, examples
activate plasminogen, plasmin; tissue plasminogen activator, urokinase, streptokinase
describe tissue plasminogen activator
initially isolated from a tumour cell line, promotes conversion of plasminogen to plasmin, selective for fibrin-bound plasminogen, low antigenicity (repeated uses)
describe streptokinase
indirect, potential allergic rx, high antigenicity, higher risk of bleeding, cheaper, plasma clearance in 15-25 min
describe the adrenal medulla, actions
modified sympathetic ganglion, innervated by preganglionic sympathetic nerve fibers, responds to sns stim in stress conditions; secretes catecholamines - epinephrine, norepinephrine
3 regions of adrenal cortex
zona glomerulosa (out) - aldosterone, zona fasciculata - hydrocortisone, zona reticularis (in) - sex hormones
what is the precursor of all adrenalcortical hormones
what does aldosterone do (what does it increase/decrease, stimulate)
stimulates renal tubules, increase Na and decrease K in blood, increase BV and BP
what factors stimulate aldosterone secretion
hyperkalemia, hyponatremia, hypovolemia, hypotension, RAS
how are glucocorticoids regulated
corticotropin releasing hormone increases adrenocorticotropic hormone or ACTH, increase glucocorticoids, -ve feedback
what does ACTH do
synthesis and secretion of glucocorticoids, growth of the adrenal gland
what is the mechanism of glucocorticoid action
cross cell membrane by diffusion, bind to receptors in cytoplasm or nucleus, activate/inactivate genes, alter rate of DNA transcription (change patterns of protein synthesis), affect metabolic activity and structure of target cell
metabolic effect of glucocorticoids
increase gluconeogenesis and blood glucose level, decrease glucose uptake and utilization by cells, increase metabolization of protein and amino acids and protein catabolism, increase mobilization of peripheral fat to face and trunk
other effects of glucocorticoids
decrease number and activity of wbcs, increase rbcs and neutrophils, decrease lymphocytes and eosinophils, Na and water retention, K excretion, increase BV and BP, mucosal ulceration, increased CNS excitability
therapeutic uses of glucocorticoids
adrenal hypofunction, allergic rxns, bronchial asthma, autoimmune diseases (rheumatoid arthritis, SLE), organ transplant, malignancies (acute leukemia), inflammatory conditions (IBD, renal disease)
what ending do glucocorticoids have, routes
one; topical, oral, inhale, inject (IM, IV, SC, intralesional)
2 adrenal gland disorders w/ examples
adrenocortical insufficiency - addison's disease; adrenocortical hyperfunction - conn's syndrome, cushing's, congenital adrenal hyperplasia
what is addison's, primary and secondary causes
hypofx of all zones of adrenal cortex; primary = adrenal gland disorder (autoimmune mediated destruction, tuberculosis, other infections, bilateral adrenolectomy); secondary = pituitary gland disorder - not enough ACTH, sudden withdrawal of long steroid therapy, trauma/tumour of pituitary gland
clinical manifestations and tx of addison's
fatigue, muscle weakness, hypotension, anorexia, n/v, abd pain, weight loss, mental depression, shock; hormone replacement (cortisol deficiency - oral hydrocortisone, aldosterone deficiency - oral fludrocortisone)
describe conn's, causes, main features
increased aldosterone secretion in absence of activation of RAS; caused by adrenal hyperplasia, adrenal tumours (adenoma, carcinoma); hypertension, hypokalemia, decreased renin level, alkalosis
describe cushings and causes
increased glucocorticoid secretion; iatrogenic (excess steroid or ACTH therapy, most common) or spontaneous (adrenal hyperplasia, adrenal tumours, excess pituitary ACTH secretion, ectopic ACTH secretion by some tumours)
clinical manifestations and tx of cushings
obesity (moon face, buffalo hump), myopathy, hypertension, hyperglycemia (diabetes mellitus), recurrent infections, thin atrophic skin w/ bruises, osteoporosis, psychosis; treat the cause
describe congenital adrenal hyperplasia, effects, clinical manifestations
congenital metabolic disorder - autosomal recessive, due to enzymatic defect; increased adrenal androgens, decreased cortisol and aldosterone; females - masculinization, males - precocious puberty
what are the gonadal hormones and what do they do
female: estrogen - develop/maintain sex characteristics, progestins - ovarian cycle, maintain pregnancy; male: androgens - develop/maintain sex characteristics
types of estrogens w/ examples
natural - estradiol; semisynthetic - ethinyl estradiol, estradiol valerate; synthetic - mestranol, stilboestrol
describe the pharmacokinetics of estrogens
absorbed through GIT, skin, mucous membranes; transported by binding to albumin or sex steroid-binding globulin; metabolized and degraded in liver (synthetic less prone); excreted through kidneys in urine
therapeutic indications of estrogens
contraception, replacement therapy (menopausal symptoms, hypogonadism), menstrual disorders, acne, prostatic cancer
what causes female hypogonadism, types, tx
impaired ovarian fx; pre-pubertal (primary, delayed puberty), post-pubertal (secondary, secondary amenorrhea and infertility); tx is small doses of estrogen
what are the effects of hyperestrogenemia in males and females
male - feminizaton, infertility, breast enlargement; females - endometrial carcinoma, breast cancer
describe 2 antiestrogens
tamoxifen - estrogen receptor blocker, tx of breast cancer; clomiphene - inhibits estrogen-mediated negative feedback on hypothalamus, tx of infertility
how does clomiphene work?
Hypothalamus makes gnrh – stimulates pituitary to make fsh and lh; these stimulate the ovaries and corpus luteum to make estrogen and progesterone which inhibit fsh and lh; clomiphene blocks this, prevents inhibition of fsh and lh; they increase and stimulate ovulation
types of progestins
natural - progesterone (from corpus luteum and placenta); synthetic - 3 generations
therapeutic indications for progestin
contraception, hormone replacement therapy, menstrual disorders, dysmenorrhea, endometriosis, endometrial carcinoma
example of antiprogestins, mechanism, indication
mifepristone; high affinity for progesterone receptor, competitive decrease of natural progesterone; therapeutic abortion
3 types of hormonal contraception
oral contraceptives (OCC), injections/implants, transdermal patch
2 types of OCC
combined OCC - estrogen and progestin, most popular, monophasic/fixed dose, bi/triphasic/variable dose; progestin minipill - low dose progestin
mechanism of estrogen-progestin combo
suppress ovulation - decrease gnrh from hypothalamus and fsh/lh from pituitary, thicken cervical secretions, inhibit implantation
mechanism of low-dose progestin
thicken cervical secretions, inhibit implantation, variable suppression of ovulation by effect on fsh/lh
adverse effects of occ
salt/water retention, edema, hypertension, vascular disorders (thromboembolic, coronary artery, cerebrovascular disease), headache/migraine, depression, postpill amenorrhea
contraindications of occ
absolute - pregnancy, breast feeding, thromboembolic disease, breast/cervical cancer, undiagnosed vaginal bleeding; relative - hypertension, impaired liver fx, migraine
types of contraceptive injections/implants
long-acting progestins; injections - IM inject ever 3m, medroxyprogesterone; implants - SC insertion of small capsules, 3-5 years, levonorgestrel
what can be done in hrt, benefits
estrogen in postmenopausal women, low dose estrogen compared to contraceptives, progestin to reduce risk of endometrial carcinoma; prevent changes associated w/ menopause (osteoporosis, flushing, headache, insomnia, genital tract atrophy, cardiovascular disease)
types of androgens
natural - testosterone, dihydrotestosterone, dehydroepiandrosterone (DHEA), androstenedione; synthetic - methyltestosterone, ethyloestrenol, stanozolol
actions of androgens
regulate gene expression by activating a nuclear receptor, develop male primary/secondary sex characteristics, maturation of sperm, anabolic effect
therapeutic indications of androgens
hormone replacement (hypogonadism, hypopituitarism), anemia refractory to tx to stimulate erythropoiesis, breast cancer, compensate for protein loss
types and tx of hypogonadism, routes
primary - testicular failure, secondary - hypothalamic-pituitary disease; androgen replacement; oral, transdermal patch, IM injection, subdermal implants
hyperandrogenemia in males and females
male - precocious puberty; female - virilization symptoms (hirsutism, acne, amenorrhea, clitoral enlargement, deep voice), masculinization of external genitalia of infants
2 types of anti-androgens, used to treat
androgen suppressors - prostatic carcinoma, endometriosis; receptor inhibitors - prostatic carcinoma, hirsutism, virilization, precocious puberty
male oral contraceptive, example, from, action, adverse effects
gossypol; from cotton plant, china; inhibits sperm production; irreversibility, hypokalemia
what is valerian
sedative and hypnotic; Contains valepotriates-- shown to have CNS depressant activity with less adverse effect than diazepam
what is echinacea
antibiotic, immune stimulant; activates T-lymphocytes to fight cold
what is St. John's Wort
contains hypericin; high conc inhibits reuptake of serotonin, norepi, dopamine in CNS; antidepressant
what is Kava
kava lactones - anti-anxiety
what are the conditions for using OTC drugs
condition is mild, not more than 2 wks, if worsening see doc, stop if adverse rxn
problems w/ aspirin
toxicity - gastric irritation, tinnitus; reyes syndrom in children w/ fever, allergic rxns
problems/plus side w/ acetaminophen
no gi irritation, no reyes, equal to asa; overdose - fatal hepatic necrosis
plus side of ibuprofen
equal to asa/tylenol, better anti-inflam
what is naproxen
anti-inflam, antipyretic, analgesic - new to market
what do cold preparations contain
antihistamines, decongestants, cough suppressant, expectorant, analgesic, antipyretic
what do antitussives do
suppress cough (codeine and dextromethorphan), suppress cough center (receptors), contain alcohol
drug of choice for hay fever prep
H1 antagonist (no combos)
what two classes of laxatives shouldn't be used
stimulant cathartics - castor oil (loss of water and electrolytes), saline cathartics - retain water in fecal mass
examples of bulk forming laxative and emollient laxative
methylcellulose (soft stool, drug of choice), dioctyl sodium sulfosuccinate (colace) - water into feces, drug induced constipation
two types of antidiarrheal agents
absorbents - attapulgite (clay, adds bulk), loperamide - synthetic opioid, traveler's diarrhea
two kinds of pancreatic glands, purpose
exocrine - produce pancreatic digestive enzymes; endocrine - hormones, clusters (islets of langerhans)
purpose of cells in islets of langerhans
alpha - glucagon, beta - insulin, delta - somatostatin, PP (F) - pancreatic polypeptide (fx uncertain)
what are the effects of glucagon
stimulate gluconeogenesis in liver, glucogenolysis (glycogen to glucose) in skeletal muscles and liver, breakdown of triglycerides in adipose tissue, fatty acid release (lipolysis)
what are the effects of insulin
accelerate glucose uptake and utilization, glycogen formation (glycogenesis), triglyceride formation (lipogenesis), amino acid absorption and protein synthesis
what is the normal blood glucose level, fasting and 2hr after meal
70-110, under 180
indications for insulin therapy
types I and II diabetes, gestational
5 different kinds of insulin preparations
ultrashort acting - lispro & aspart, short - regular (crystalline), intermediate - NPH & lente, long - ultralente, mixed types
name 5 oral hypoglycemics (classes)
sulfonylureas, biguanides, meglitinides, thiazolidinedones, alpha-glucosidase inhibitors
mechanism of action of sulfonylureas
stimulate insulin secretion by beta cell (inhibit K channels on b cell, depolarize, Ca enters, insulin released), only good for type II
pharmacokinetics of sulfonylureas
bind to plasma proteins, metabolized in liver, excreted through kidneys, exaggerated in elderly and renal/liver disease, cross placenta
examples of 3 generations of sulfonylureas drugs
1 - tolbutamide, chlorpropamide 2 - glipizide, glibenclamide, Ggliclazide 3 - glimepiride
mechanism, indication, advantage, example of biguanides
decrease gluconeogenesis, increase glucose uptake by skeletal muscles; obese pts w/ type II; no hypoglycemia b/c they don't alter insulin; metformin
mechanism, indication, side effect, example of meglitinides
similar to sulfonylureas; type II; hypoglycemia; repaglinide, nateglinide
mechanism, indication, side effects, example for thiazolidinedion (TZDs)
activate transcription regulator (PPARy) - modulate lipogenesis, improve glucose uptake, improve insulin effect; type II; heart failure, myocardial ischemia, liver injury; rosiglitazone
mechanism, side effects, example of alpha-glucosidase inhibitors
inhibit a-glucosidase in intestine, reduce absorption of carbs, control glucose levels; GI upset, flatulence; acarbose
tonic colonic (gran mal) seizure drugs
Valproic acid (valproate)
absence/petit mal seizure drugs
Valproic acid (valproate)
myoclonic seizure drugs
Valproic acid (valproate)
status epilepticus drugs
Diazepam (i.v.)
Phenytoin (i.v.)
partial (focal) seizures, Simple, Complex (Psychomotor epilepsy)
Valproic acid (valproate)
what are some strategies for suppressing excitation of glutamate neurons
increase inhibition to neuron to suppress firing (increase GABA firing), block electrical activity of nerve to slow nerve impulses, block glutamate receptors so wave of excitation cannot spread
problem w/ phenytoin
fetal hydantoin syndrome, similar to fetal alcohol syndrome, avoid in women of child-bearing age
5 components of anesthesia
loss of consciousness, loss of memory, response to pain, autonomic response, skeletal muscle relaxation
mechanism of action of general anesthesia
global depression of CNS, depression of RAS (reticular activating system), lipid matrix expansion, GABA mediated inhibition at GABAa receptor chloride channel, antagonism of glutamic acid excitation of NMDA channel receptor
3 phases of general anesthetic
induction - render pt unconscious; maintenance - maintain unconsciousness, analgesia, muscle relaxation; emergence - elimination/metabolism of drug, antagonsim
what is MAC
minimum alveolar concentration - concentration of inhaled anesthetic required to prevent 50% of pts from responding to painful stimulus; Way to compare and measure various volatile agents; high MAC = low potency like nitrous oxide
name/describe volatile anesthetics
desflurane, sevoflurane, isoflurane, halothane; liquid at room temp, potent - need vaporizer, decrease bp and resp, bronchial dilation
signs and symptoms/tx of malignant hyperthermia
muscle rigidity, tachycardia, acidosis, hypercarbia, hypoxemia, hyperthermia; stop agent, give O2, dantrolene, treat acidosis, cool, support vitals
describe IV anesthetic propofol
rapid offset, hypotension, apnea, prevents n/v, ideal ambulatory anesthetic
describe IV anesthetic etomidate
block of norepi uptake, no change in bp or hr, apnea, n/v, adrenocrotical suppression; good for hemodynamic compromise
describe IV anesthetic ketamine
recreational street drug, hypertension, tachycardia, usually no apnea, provides analgesia, high intracranial pressure, dysphoria, good for hemodynamic compromise
2 kinds of local anesthetics and examples (amino ____)
amino esters - procaine, tetrocaine, cocaine; amino amides - lidocaine, bupivacaine, ropivacaine
how do local anesthetics work
blockage of voltage gated sodium channels; block nerve transmission and autonomic fx, temp sensation, light touch sensation, proprioception, motor fx
what is the rule about local anesthetics and potency
more lipid soluble = more potent
describe the two ways alcohol is metabolized
alcohol dehydrogenase - rate limiting (due to coenzyme NAD), hangover; MEOS when alcohol dehydrogenase is saturated
describe the pharmacokinetics of alcohol
95% metabolized/biotransformed, primarily in liver, smaller amount in stomach, rest is excreted in breath, urine, sweat; zero-order kinetics - rate of oxidation is independent of time and concentration
why do women have higher peak alcohol concentrations for equal dose
lower levels of gastric alcohol dehydrogenase, lower muscle-to-fat ratio, concentrate alcohol in plasma more due to higher fat content
describe the pharmacodynamics of alcohol
CNS depressant, inhibits NMDA receptor activity, activates GABA-mediated neuronal transmission leading to inhibition
what is wernickes encephalopathy (inadequate amount of what?)
ataxia - lack of coordination, confusion, impairment of short term memory; inadequate intake/absorption of thiamine
what is korsakoffs psychosis
anterograde amnesia - no new memories, severe memory loss, confabulation, meager content in conversation, lack of insight/apathy; deficiency of thiamine
3 txs for alcoholism
naltrexone - opioid receptor antagonist; acamprosate - weak NMDA-receptor antagonist, GABAa-receptor activator; disulfiram - inhibits acetaldehyde dehydrogenase leading to accumulation of acetaldehyde (hangover)
describe alcohol withdrawal
excitability of CNS, convulsions/coma/death, delirium tremens - hallucinations, confusion, psychomotor agitation, disorientation, sleep disorders
3 diagnostic features of FAS
growth restriction, craniofacial dysmorphology, CNS dysfunction
5 classes of antimicrobial agents
antibacterials, antiviral, antifungal, antiprotozoal, antihelmenthics
3 types of bacteria morphology
cocci-circle, bacilli-rod, spiral-spirochete
penicillin G is an example of what kind of antibiotic
narrow spectrum gram + cocci
aminoglycosides are an example of what kind of antibiotic
narrow spectrum gram - bacilli
tetracyclines are an example of what kind of antibiotic
broad spectrum gram +/-
two different effects of antibiotics w/ examples
bacteriostatic - inhibit growth/repro, tetracyclines, sulphoamides; bactericidal - kill bacteria, penicillins, cephalosporins
two examples of synergistic effects of antibiotics
sulfonamides + trimethoprim; clavulanate + amoxicillin (one drug prevents inactivation of the second)
ex of an antagonistic effect of antibiotics
tetracycline inhibits action of penicillin
6 examples of antibiotics (classes)
penicillin, cephalosporins, tetracyclines, aminoglycosides, sulphonamides, quinolones
what is the structure of penicillins
core of 6-aminopenicillanic acid, B-lactam ring (active), + side (R) group (determines type)
mechanism of action of penicillin (mainly gram + or -?)
bactericidal, inhibit formation of peptidoglycan cross-links in bacterial cell wall, mainly gram + bacteria (some exceptions)
describe penicillin resistance
destruction by B-lactamase enzyme - synthesized by certain bacteria (staphylococci)
how is penicillin resistance avoided
clavulanic acid - potent inhibitor of B-lactamase, combined w/ some penicillins (amoxicillin); B-lactamase resistant penicillin (coloxacillin, dicloxacillin, methicillin)
5 types of penicillin
penicillin G, penicillin V, benzathine benzylpenicillin, B-lactamase resistant penicillin, broad spectrum penicillin
what spectrums do the 4 classes of cephalosporins cover
first gram +, second gram - w/ some +, third broad spectrum w/ more gram -, fourth broad spectrum w/ more +
mechanism of action of tetracyclines and aminoglycosides
Inhibition of protein synthesis through binding to 30S ribosomal subunit
mechanism of action of sulfonamides
reversible competitive, prevent making folic acid
mechanism of action of quinolones
Inhibit bacterial topoisomerase II (DNA gyrase) enzyme (required for transcription and DNA replication)
indication, example, other facts about quinolones
complicated UTI, serious gram - infections, broad spectrum, some are discontinued, saved for serious ones b/c of side effects; ciprofloxacin
what does current theory suggest the cause of depression is
reduction in activity of one or more neurotransmitter systems in the CNS regions essential to regulating emotions - norepinephrine, serotonin, dopamine?
4 treatments for depression
SSRIs, tricyclic antidepressants (TCAs), monoamine oxidase inhibitors (MAOIs), presynaptic autoreceptor blockade, electroconvulsive therapy (ECT)
examples of drug names of SSRIs
Fluvoxamine, Fluoxetine, Paroxetine, Sertraline, Citalopram, Escitalopram
problems w/ SSRIs
withdrawal symptoms- discontinuation syndrome; inhibit cytochrome P450 - inhibit drug metabolism, toxicity; serotonin syndrome
common drug names of TCAs
Imipramine, Amitriptyline, Desipramine, Nortriptyline, Clomipramine
problems w/ TCAs
anticholinergic, antihistaminergic, block a1 adrenergic receptors, block sodium channels
MAOI examples
Phenelzine, Tranylcypromine, Moclobemide
problems w/ MAOIs
hypo/hypertension, agitation, insomnia, food interactions can be fatal - tyramine leads to hypertensive crisis; serotonin syndrome, hyperpyrexic crisis w/ opiates, hypertensive crisis w/ stimulant meds
two-step process to treat mania
antipsychotic to reduce mood to normal range (Haloperidol, Chlorpromazine, New Atypical Antipsychotics), mood stabilizer to keep it there
mood stabilizer drug names examples
lithium, valproic acid (valproate, divalproex), carbamazepine, atypical antipsychotics (Olanzapine, Risperidone, Quetiapine, Ziprasidone)
4 major classes of antineoplastics
antimetabolites, antimitotics, alkylating agents, topoisomerase inhibitors
mechanism of antimetabolites
analogues of purines & pyrimidines - competitive decrease of these metabolites to interfere w/ RNA/DNA synthesis, arrest growth and division of malignant cells during S phase of interphase
3 classes of antimetabolites
purine analogues - 6-mercaptopurine; pyrimidine analogues - 5-fluorouracil, cytosine arabinoside; antifolates - methotrexate
mechanism of methotrexate
folic acid analogue - decreases DHFR enzyme, decrease THF (essential for purine/pyrimidine bases)
examples of antimitotics
vinca alkaloids - vincristine, vinblastine; taxanes - taxol
mechanism of antimitotics
bind to tubulin, decrease polymerization, prevent microtubule formation (vinca alkaloids); stabilize microtubules, prevent separation of chromosomes (taxol)
mechanism of alkylating agents
attach an alkyl group to DNA, cross-link DNA strands, strands unable to uncoil, abnormal base-pairing, DNA damage and cell death
3 types of alkylating agents
nitrogen mustards - cyclophosphamide, chlorambucil; ntirosureas - carmustine; platinum-based drugs - cisplatin
mechanism of topoisomerase inhibitors
block DNA ligation, DNA breaks, interrupt protein synthesis and cell division, apoptosis
types of topoisomerase inhibitors
topoisomerase I inhibitors - inrinotecan; topoisomerase II inhibitors: antineoplastics -doxorubicin, etoposide antibiotics - quinolones
4 other antineoplastics
antitumor antibiotics - interfere w/ RNA/DNA, actinomycin, bleomycin; hormones - selective suppression of tumour cells, tamoxifen; retinoids - vit A analogues, stimulate apoptosis, fenretinide; antiangiogenic agents - interfere with neovascularization
what is a genetic protective factor for alcoholism?
single point mutation for aldehyde dehydrogenase; excessive drinking increases acetaldehyde levels causing vasodilation
name 3 isoenzymes of cyclooxygenase enzyme
cox-1 (widely distributed, kidney), cox-2 (limited distribution, inflammation), cox-3 (mainly in brain, slightly different)
3 types of antipyretics
NSAIDs (ASA, ibuprofen), Acetaminophen, selective cox-2 inhibitors (celecoxib)
mechanism of action of ASA
irreversible inhibition of cox-1 and 2, decrease production of prostaglandins and thromboxanes
how does ASA reduce pain, fever, thromboembolic disease
inhibition of PG synthesis, prevents sensitization of pain-transmitting nerve fibres to chemical mediators released by tissue injury, inhibits action of transmitters involved in pain pathways; reset temp center in hypothalamus; antiplatelet effect
reyes syndrome associated w/ ASA
brain/liver damage can be fatal, children/adolescents who have viral infection and take aspirin
mechanism of action of acetaminophen
not fully understood, inhibits cox enzyme
name classes of drugs w/ examples for anxiety/sleep disorders
barbiturates (phenobarbital), benzodiazepines (diazepam, pams), Buspirone, Z drugs (zopiclone), serotonin re-uptake inhibitor antidepressants
how is CNS neurotransmission controlled (what controls its excitability?)
GABA neurons control CNS excitability by suppressing glutamate nerve firing
mechanism of benzodiazepines
promotes GABA - BZ1 (inhibition sleep/wake part of CNS), BZ2 (inhibition of other parts of CNS)
what are the 3 categories of benzodiazepines
short (oxazepam, lorazepam), intermediate, long acting (diazepam)
3 ways to increase serotonin to reduce anxiety (what is a precursor for it?)
serotonin agonist (buspirone), serotonin reuptake inhibitor antidepressants, dietary tryptophan (precursor amino acid)
2 classifications of analgesics
narcotic analgesics (opioids) and non-narcotic analgesics (antipyretics)
4 types of opioids w/ examples
endogenous (endorphines), plant alkaloids (morphine, codeine, thebaine), semisynthetic (diamorphine/heroin, hydromorphine), synthetic (pethidine/meperidine, methadone, fentanyl)
two types of opioid antagonists w/ examples
antagonists - naloxone, mixed agonists/antagonists - pentazocine
therapeutic use of naloxone
tx of opioid drug overdose (antidote), dx and tx of opioid dependence, should be available when opioid drugs are run through IV
how is opioid dependence treated
methadone, buprenorphine, naloxone