exam Flashcards
1
Q
Aspirin (low doses: antiplatelet (50-150 mg), high doses: antiinflammatory (500-1000mg))
A
A= NSAID, salicylate ester of acetic acid, antiplatelet, analgesic, antipyretic B= inhibits COX-1 and COX-2 activity. Irreversible acetylates and inactivates COX1 in platelets (Low doses) ---> inhibits synthesis of thromboxane A2 which is necessary for platelets to change their forms and release granules which leads to platelet aggregation. (In high doses also acts on COX enzymes in the endothelium--> blocks their action and subsequently decreases amount of inflammatory mediators & prostaglandins) C= TIA, stroke, primary and secondary prevention of CAD and MI, embolism ass with atrial fibrillation/flutter.
2
Q
Adrenaline/Epinephrine
A
A= adrenopositive drug, alpha and beta agonist, direct acting sympathomimetics B= binds to and activates alpha1-2 and beta 1-2 receptors non-selectively --> evokes sympathetic effects(positive ino-batmo-dromo-chronotrophic effects on heart, systemic vasoconstriction, GIT relaxation, dilates bronchi and cerebral vessels). C= cardiopulmonary resuscitation, acute anaphylaxis, angioedema, cardiac arrest, acute asthmatic effects, stokes-Adams syndrome
3
Q
Alendronic acid/ sodium alendronate
A
A= second generation bisphosphonate, nitrogen-containing agent B= inhibits FPP (farnesyl pyrophosphate synthase) synthase enzyme in osteoclasts which prevents the biosynthesis of isoprenoid lipids (FPP) which further prevents osteoclastic activity and reduces bone resorption and turnover. (Mevalonate pathway). In postmenopausal women it reduces he elevated rate of bone turnover leading to a net gain in bone mass C= osteoporosis, Paget's disease, hypercalciemia, bone metastases
4
Q
Aminophylline
A
A= metylxanthine derivative, bronchodilator, theophylline derivative B= after ingestion, theophylline is released which relaxes the SMC of bronchi and pulmonary bv, reduces airway responsiveness to histamine, adenosine and allergens--> phosphodiesterase inhibitor, adenosine receptor blocker, histone deacetylase activator C= asthma, chronic bronchitis, COPD
5
Q
Amiodarone
A
A= class 3 antiarrhytmic drug B= prolongs APD (repolarization and QT interval) by blocking Ikr channels. During chronic administration also blocks Iks channels. Also inactivates Na+ channels and has weak adrenergic and calcium channel blocking properties --> slowing of HR and AV conductance due to all its combined actions C= maintenance of normal sinus rhythm in patients with afib, supraventricular arrhytmias, prevention of ventricular tachycardia, ventricular arrhytmias
6
Q
Amitriptyline
A
A= sedative TCA (NSRI) B= blocks both SER and NE reuptake transporters + blocks H1, H2, muscarinic and presynaptic alpha receptors that normally would inhibit release of NE and SER --> increases the availability of NE and SER in the synaptic cleft C= depressive illness where sedation is needed, endogenous depression, reactive depression, manic-depressive syndrome (depressive phase) panic disorders, severe anxiety, phobias + neuropathic pain, migraines when used as co-analgesics (prophylaxis), incontinence (not first line) und
7
Q
Amlodipine
A
A= calcium channel blocker, 3rd generation dihydropyridine derivatives B= blocks voltage gated vascular alpha1 subunit of L-type calcium channels, decreases I/c levels of calcium in vascular smc, decreases contraction, cause muscle relaxation and vasodilation (reduces vascular resistance) C= hypertension, angina pectoris, anti arrhythmiac
8
Q
Aripiprazole
A
A= Newer antipsychotic preparation, atypical antipsychotic B= a combination of antagonism at D2 (partial agonist) receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia. Also some alpha2 receptor block C= Schizophrenia and psychosis (acute and chronic forms), bipolar disorders (manic phase), agitation in Alzheimers and Parkinsons, major depression disorder
9
Q
Atorvastatin
A
A= statins (flourine containing) B= competetive inhibitor of HMG coA reductase -> reduced cholesterol synthesis and up regulate LDL receptors on hepatocytes --> decreases LDL levels +modest reduction in triglycerides C= treatment of dyslipidemia, prevention of cardiovascular diseases and MI, antifibrotic and anti inflammatory effects on vessel wall, anti oxidant (=stabilizes the fatty plaque), acute coronary syndrome!(Atherosclerotic vascular disease (primary and secondary prevention +acute coro- nary syndromes)
10
Q
Atropine
A
A= cholinonegative drug (direct acting), competitive nonselective muscarinic antagonist (tertiary amine alkaloid ester) B= binds to and prevents activity of all muscarinic receptors=> reversable blockade of Vagal nerve=> oppose parasympathetic effects: increases heart action (prevents bradycardia and asystole), suppressed sweating, bronchodilatation C= Parkinson's disease (reduces tremor and rigidity), intoxication and poisoning treatment of mushrooms and muscarinic agonists, eye treatment (dilating pupil/mydriadis and cytoplegia! , bradycardia and first line treatment for heart block, premedication (reduces hyper secretion of airway glands).
11
Q
Bevacizumab
A
A= recombinant monoclonal IgG1 antibody, anticancer drug, antiangiogenic drug B= inhibits binding of VEGF-A to VEGFR leading to inhibition of VEGF signaling+ inhibits tumor vascular permability and inhibits angiogenesis in tumors C= colorectal cancer, breast cancer, non-small cell lung cancer, renal cell cancer
12
Q
Bisacodyl
A
A= synthetic stimulant laxative B= directly stimulate colonic nerves that will cause movement of faecal mass, reduce transit time and result in the passage of stool within 8-12 hours (increases intestinal motility). It's hydrolyzed by intestinal brush border enzymes and colonic bacteria to form an active metabolite that acts directly on the colonic mucosa to produce colonic peristalsis. Also increases water and electrolytes in feces C= relief of constipation and management of neurogenic bowel dysfunction, bowel prep for medical examinations
13
Q
Bisoprolol
A
A= adrenonegative drug, cardioselective beta1 blocker without ISA + Class 2 antiarrhytmic drug B= blocks beta1 receptors in heart and vascular smooth muscle. This results in a reduction of HR, CO, bp etc. At higher doses (>20mg) Bisoprolol may completely block beta2 receptors in bronchial and vascular smooth muscles --> bronchospasm and vasodilation. Also decreases renin levels C= angina pectoris, hypertension, tachycardia, migraine,coronary artery disease, ischemic heart diseases, prevention of MI
14
Q
Bromazepam
A
A= Benzodiazepine, anxiolytic (daily tranquilzer) B= acts at GABAa receptors and facilitates its release in CNS--> facilitating frequency of GABA-mediator chloride ion channel opening--> enhancing membrane hyperpolarization -->depressant effects of CNS including sedation and relief of anxiety, amnesia, hypnosis, anesthesia, coma and resp depression C= acute anxiety states, panic attacks, generalized anxiety disorder, insomnia and other sleeping disorders, relaxation of skeletal muscle, anesthesia, seizure disorders
15
Q
Bupivacaine
A
A= local anaesthetics, amide type, B= prevents transmission of impulses along nerve fibers and at nerve endings by causing reversable blockade of sensory receptors and decreasing permeability of ions (potassium and sodium) C= infiltration anaesthetics, regional anesthesia for surgery, dental surgery, for diagnostics and therapeutic procedures, obstetrical procedures (epidural infusions used for postoperative pain con- trol and for labor analgesia)
16
Q
Carbamazepine
A
A= 1st line tricyclic antiepiletic drug B= inhibits uptake and release of NE, blocks Na+ and ca2+ channels which subsequently will increase the threshold for glutamate release-->decreases synaptic transmission and therefore inhibits the repetetive high frequency firing of neurons. C= generalized tonic-clonic (grand mal) seizures, partial seizures (almost all types except absence seizures), prophylaxis of manic-depressive illness in patients unresponsive to lithium/diazepam (bipolar disorders), trigeminal neuralgia and diabetic neuropathies
17
Q
Clomiphen
A
A= anti-estrogen, SERM (selective estranged receptor modulator) B= stimulates ovulation by affecting the negative feedback and therefore cause FSH and LH release. Clomiphen is a partial agonist at estrogen receptors --> increases the secretion of the gonadotropins and Gnrh and estrogens by inhibiting estradiols negative feedback on the gonadotropins C= infertility, induction of ovulation (anovulation), POS, oligomenorrhoea/amenorrhoea
18
Q
Clonidine
A
A= adrenopositive drug, selective alpha2 presynaptic receptor agonist (neurotropic drug) B= binds to and activates presynaptic alpha2 receptors --> located on cardiovascular control centers--> decreasing impulsation among sympathetic nerves from CNS--> decreasing of bp. Blood vessels--> decreased release of NE and decreasing of bp. Also binds to and activates I1 receptors (imidazoline receptors) which mediates sympathonegative actions to lower blood pressure C= hypertension, hypertensive crisis when immideate effects are not necessary. Differential diagnosis of pheochromocytoma in hypertensive patients, prophylaxis of vascular migraine headaches, ADHD. Painkiller properties, reliefs withdrawal symptoms of opioids or alcohol abuse
19
Q
Clopidogrel
A
A=Antiplatelet B= the active metabolite binds selectively and noncompetitively to platelet surface P2Y12 ADP receptors, therefore inhibits ADP from bindint to the receptor and subsequent receptor activation of the platelet glycoprotein (GP IIb/IIIa) complex which is necessary for fibrinogen-platelet binding. Also inhibits ADP-mediated release of granules required for platelet aggregation C= to avoid thrombosis in patients with coronary stent placement, unstable angina, NSTEMI in combination with aspirirn, STEMI, recent MI, stroke, peripheral arterial disease,
20
Q
Dabigatran
A
A= oral anticoagulant, synthetic thrombin inhibitor B= D is a rapid-acting competitive and reversible direct inhibitor of thrombin. Thrombin, a serine protease, is responsible for the conversion of fibrinogen to fibrin in the coagulation cascade. Inhibition of thrombin consequently prevents thrombus development. Dabigatran inhibits free thrombin, fibrin-bound thrombin and thrombin-induced platelet aggregation. C= prevention of strokes in afib due to non heart valve causes. DVT, PE (prevention of venous thromboembolism in patients undergoing hip replacement surgery)
21
Q
Desmopressin
A
A= vasopressin receptor agonist, synthetic analogue of ADH B= binds to and agonizes vasopressin2 receptors in the nephrons of collecting ducts to decrease excretion of water (ADH effect) + agonizes extrarenal V2 receptors to increase levels of factor VIII and vWF C= nocturnal enuresis, control of temporary polyuria and polydipsia following trauma/injury in pituitary region. Pituitary diabetes insipidus, hemophilia A and von Willebrand disease
22
Q
Dextromethorphan
A
A= centrally acting, non narcotic antitussive, opioid derivative (partial u opioid receptor agonist) B= reduces cough reflex by acting centrally on the respiratory centre in the medulla and nucleus tractus Solaris (increases the cough threshold). As a NMDA-receptor antagonist exert some anaesthetic functions C= acute coughing, temporary relief of coughs, colds, allergies, inhaled irritants
23
Q
Diazepam (Valium)
A
A= Benzodiazepine, anxiolytic (major tranquilzer) B= acts at GABAa receptors and facilitates its release--> reduces spasticity by increasing interneuron inhibition of primary motor afferents in spinal cord and CNS (Bind to specific GABAA receptor subunits at central nervous system (CNS) facilitating frequency of GABA-mediated chloride ion channel opening—enhance membrane hyperpolariza- tion) C= general anesthesia induction, anxiety, seizures (muscle relaxant, used in status epilepticus), alcohol withdrawal, insomnia, chronic muscle spasms due to cerebral palsy, strokes, acute spinal cord injury
24
Q
Diclofenac (voltaren)
A
A= NSAID, analgesics, antipyretics, phenylacetic acid derivative, non-selective COX inhibitor B= nonselectively inhibits both COX1 and COX2 + inhibits leucocyte migration --> inhibits prostaglandin synthesis from arachidonic acid C= osteoarthritis, rheumatoid arthritis, used as a painkiller e.g. in pain induced by dysmenorrhea, ocular inflammation, ankylosing spondylitis, solar keratosis, acute gout, postoperative pain, poly arthritis, fibromyalgias, arthrosis, fever
25
Q
Digoxin
A
A= cardiac glycoside, digitalis, class 5 antiarrhytmic B= inhibits Na+/K+/ATPase membrane pump--> increase in i/c Na+ levels (and decrease I/c K+ levels). The NCX in turn tries to extrude the sodium and in doing so, pumps in more calcium. Increased ca2+ levels promotes activation of contractile proteins of cardiac sarcomere--> increases cardiac contractility (positive inotrophic and little batmotropic effects) cardiac parasympathomimetic effects (slowed HR, slow AV conduction). Also shortens APD (by increased potassium conductance due to increased i/c calcium levels) and decreasing the maximal diastolic potential C= chronic heart failure, rapid ventricular rate in afib, congestive cardiac insufficiency, arrhytmias
26
Q
Diltiazem
A
A= non-DHP calcium channel blocker, class 4 antiarrhytmic drug B= blocks L type calcium channels--> inhibits influx of e/c calcium across myocaridum and vascular SMC--> reduces cardiac rate and output(negative chrono and dromotropic effects), reduces peripheral vascular resistance C= hypertension, angina, supraventricular tachycardia and arrhytmias
27
Q
Dinoprost
A
A= synthetic PGF2alpha B= stimulates contraction of the uterus in myometrium (via its interaction with pg receptors) and directly affects collagenases in the uterus as well as increases proteoglycan content resulting in softening of the cervix C= induces abortion during 2nd trimester, for missed abortion, for benign hydatidiform mole and is also used for ripening of the cervix for induction of labor in patients at or near term
28
Q
Dobutamine
A
A= adrenopositive drug, selective beta1 receptor agonist B= activates mainly beta1 receptors of heart--> increased cAMP(thru the action of adenylyl cyclase)--> increases contractility with little effect on heart rate and beta2 receptors--> increases CO. Does not Cause release of NE as dopamine C= used in case of inotrophic support in cardiomyopathies, septic shock, cardiogenic shock, acute decompensated heart failure, intermittent therapy in chronic heart failure reduces the symptoms
29
Q
Dopamine
A
A= adrenopositive drug, alpha and beta agonist B= activates alpha1 and beta1 receptors--> causes positive chronotropic and inotrophic effects on myocaridum --> increased HR and contractility--> due to directly activating beta adrenergic receptors and indirectly due to causing release of NE from storage sites of sympathetic neurons. In the brain dopamin acts as an agonist to be 5 receptor subtypes (d1-5) C= cardiogenic shock in infarction or cardiac surgery. Hemorrhagic shock, shock due to renal failure
30
Q
Doxazosin
A
A= adrenonegative drug, selective alpha1 antagonist B= blocks selectively alpha1 receptors --> decreases systemic peripheral vascular resistance (alpha1b receptors) and induces vasodilation --> decreases bp (long lasting, 1 tab/day) also relaxes smooth muscles in urinary passages (alpha 1a receptors, decreases the resistance to urine flow) C= hypertension and benign prostatic hyperplasia
31
Q
Doxorubicin
A
A= anthracycline antibiotic, intercalating drug antitumor B= oxygen free radicals bind to DNA causing single- and double-strand DNA breaks, binds to cellular membranes to alter fluidity and ion transport, inhibits topoisomerase II, binds to DNA through intercalation with consequent blockade of DNA and RNA synthesis, DNA strand scission, C= Breast cancer, Hodgkins and non-hodgkins lymphoma, soft tissue sarcoma, ovarian cancer, non-small cell and small cell lung cancer, thyroid cancer, wilms tumor, neuroblastoma, cancers of testicles, stomach, bladder, liver
32
Q
Enoxaparin
A
A= anticoagulant, low molecular weight heparin B= has less effect on thrombin than unfractioned heparin. binds to and accelerates the activity of antithrombin III. By activating antithrombin III, enoxaparin preferentially potentiates the inhibition of coagulation factors Xa and IIa. Factor Xa catalyzes the conversion of prothrombin to thrombin, so enoxaparin’s inhibition of this process results in decreased thrombin and ultimately the prevention of fibrin clot formation. C= Hip/knee replacement surgery, general surgery thromboprophylaxis, medical conditions associated with thromboembolism, deep-vein thrombosis and pulmonary embolism, myocardial infarction
33
Q
Escitalopram
A
A= SSRI (selective) B= allosterically inhibits SERT --> inhibits SER reuptake -> increases its availabilty in the synapse C= major depressive syndrome, GAD, PTSD, OCD, panic disorder, PMDD, bulimia
34
Q
Ephedrine
A
A= adrenopositive drug, indirect sympathomimetics B= acts through the release of stored catecholamines (incl dopamine and serotonin) C= stimulate, have a stimulant effect on mood and alertness and a depressant effect on appetite. Ephedrine is utilized when prolonged duration of effect is desired, particularly after oral administration in case of nasal congestion, sinusitin and also urinary incontincence and asthma
35
Q
Etoricoxib
A
A= NSAID, antipyretics, analgesics, sulfonamide compound, selective COX2 inhibitor (less GIT side effects) B= selectively blocks COX2 enzymes --> decreases the synthesis of prostaglandins from arachidonic acid without interfering with COX1 enzyme, thus avoiding side effects better than other NSAIDS C= osteoarthritis, RA, acute pain, painful dysmenorrhea, ankylosing spondylitis, familial adenomatous polyposis, goutt
36
Q
Ezetimibe
A
A= lipid lowering drug, cholesterol absorption inhibitor B= blocks sterol transporter NPCILI in intestine brush border, inhibits re absorption of cholesterol (decreasing exogenous levels of cholesterol) decreases LDL and phytosterols levels C= elevated LDL, phytosterolemia, CAD
37
Q
Finasteride
A
A= specific 5alpha-reductase inhibitor, antiandrogen B= inhibits type II 5alpha reductase through the formation of a stable complex with this enzyme --> decreases concentrations of dihydrotestosterone (blocks the conversion of testosterone) C= benign prostatic hyperplasia, androgenetic alopecia
38
Q
Fluorouracil
A
A= pyrimidine analog, antineoplastic antimetabolite B= inhibits thymidylate synthetase, interfering with the synthesis of DNA and RNA. These effects are most marked in atypical, rapidly proliferating cells C= topical treatment for multiple actinic keratoses, colorectal cancer, breast cancer, gastroesophageal cancer, head and neck cancer, hepatocellular cancer
39
Q
Furosemide
A
A= antihypertensive drugs, loop diuretics, fast acting diruetics B= acts on the thick portion of the ascending limb of henleys loop, where they inhibit Na+/K+/2CL- cotransporter. As a result, these electrolytes, together with water, are excreted in larger amounts. Also cause vasodilation of veins and kidneys blood vessel --> mechanically decreasing blood pressure C= acute heart faiulre, severe hypertension, pulmonary oedema, cerebral oedema, oliguria due to renal failure, hypertensive crisis, hypercalcemia
40
Q
Glyceryl trinitrate/nitroglycerin (acute/short acting) sublingual
A
A= organic nitrates, anti-anginal B= free nitrate ions are released -> converted into NO which activates enzyme guanylate Cyclase -> increases I/c cGMP --> dephosphylation of myosin chain of SMC (decreases ca2+ levels) -> muscle relaxation and vasodilation& reduction of venous return -> reduction of left ventricular work and improves coronary blood flow & decreases myocardial oxygen demand (more venous tone than arterial) C= angina treatment, hypertensive crisis
41
Q
Haloperidol
A
A= Butyrophenone derivative, Long-acting typical antipsychotic agent, B= blocks central dopamine D2 receptors --> reduces vocal and motor tic frequency and severity. Also some alpha blockade and minimal M receptor blockade C= used in both acute and chronic cases of psychosis huntingtons disease, dystonia, tourettes syndrome, schizophrenia, bipolar disorder (manic phase), ballism, delusional disorders,nonpsychiatric antiemesis, peroperative sedation, pruritus
42
Q
Hydrochlorothiazide
A
A= antihypertensive drugs, thiazide-type diuretics B= acts on the distal convulated tubules of kidneys and inhibits the sodium-chloride symporter leading to retention of water in the urine (inhibits sodium reabsorption). In this way, blood plasma volume is reduced, and thus blood pressure is reduced (due to decreased preload) C= Heart failure, hypertension, oedema, nephrogenic diabetes insipidus, nephrolithiasis
43
Q
Infliximab
A
A= chimeric IgG1 anti-TNF monoclonal antibody, biological DMARD B= complexes with TNFalpha and prevents its interaction with p55 and p75 cell surface receptors--> downregulation of mph and Tcell function C= RA, ankylosing spondylitits, psoriatic arthritis, chrons disease, psoriasis, ulcerative colitis, juvenile chronic arthritis, wegners granulomatosis, giant cell arteritis, sarcoidosis
44
Q
Interferon alpha
A
A= antiviral, immunomodulating agent, antiproliferative, 2nd generation interferon B= inhibits viral penetration, translation, transcription, protein processing, maturation and release + increases phagocytic activities of mphs and augmentation of proliferation and survival of cytotoxic Tcells and NK cells C= neoplasms treatment; hairy cell leukemia, chronich myelogenous leukemia, malignant melanoma, Kaposi's sarcoma, HBV, HCV, renal cell carcinoma, carcinoid syndrome, Tcell leukemia, condylomata acuminata
45
Q
Insluin lispro
A
A= fast acting and short acting semisynthetic insulin
B=binds insulin receptors on cells and activates them –> reduces circulation glu levels and promotes glucose transport and oxidation. Influences glycagon, lipid, CH and protein metabolism and synthesis
C= diabetic ketoacidosis, DM 1,2
46
Q
Irbesartan
A
A= non-peptide tetrazole derivative, ARB, antihypertensive, B= selective competetive antagonist of angiotensin AT1 receptors--> arteriolar dilataiton, decreased aldosterone secretion--> increased sodium and water excretion, reduction in secretion of vasopressin--> decrease of bp C= hypertension, diabetic nephropathy, congestive heart failure
47
Q
Iron (III) saccharate
A
(((used for IV iron replacement))))
A= iron preparation
B= iron preparation
C= prevention and treatment of iron deficiency; treatment of iron deficiency anemia, treatment of latent anemia, anemia during pregnancy
48
Q
Isosorbide Mononitrate (active metabolite of dinitrate)
A
A= organic nitrate, anti-anginal B= free nitrate ions are released -> converted into NO which activates enzyme guanylate Cyclase -> increases I/c cGMP --> dephosphylation of myosin chain of SMC -> muscle relaxation and vasodilation& reduction of venous return -> reduction of left ventricular work and improves coronary blood flow & decreases myocardial oxygen demand C= angina prophylaxis due to CAD
