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
Digoxin
```
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
Diltiazem
```
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
Dinoprost
```
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
Dobutamine
```
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
Dopamine
```
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
Doxazosin
```
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
Doxorubicin
```
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
Enoxaparin
```
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
Escitalopram
```
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
Ephedrine
```
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
Etoricoxib
```
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
Ezetimibe
```
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
Finasteride
```
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
Fluorouracil
```
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
Furosemide
```
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
Glyceryl trinitrate/nitroglycerin (acute/short acting) sublingual
```
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
Haloperidol
```
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
Hydrochlorothiazide
```
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
Infliximab
```
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
Interferon alpha
```
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
Insluin lispro
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
Irbesartan
```
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
Iron (III) saccharate
(((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
Isosorbide Mononitrate (active metabolite of dinitrate)
```
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
```
49
Isotretinoin
```
A= synthetic retinoid (vitA)
B= inhibits sebaceous gland size and function, It also reduces inflammation in moderate-severe inflammatory acne. Thought to act through RAR receptors--> synthesis of certain proteins that reduces sebaceous gland production and inhibits keratinization
C= severe nodular acne vulgaris
```
50
Latanoprost
```
A= long acting prostanoid analog, PGF2alpha
B= decreases intraocular pressure by increasing the outflow of aqueous fluid through selective agonism at FP receptors located in the eye
C= open-angle glaucoma, ocular hypertension
```
51
Levodopa + benserazide
```
A= dopamine precursor+ peripheral DOPA decarboxylase inhibitor
B= allows levodopa to cross the blood brain barrier (as dopamine does not) and benserazide inhibits the metabolism of levodopa to dopamine peripherally (not centrally where Levodopa is then metabolized to dopamine)
C= parkinsons disease
```
52
Levonorgestrel
A=emergency contraceptive, steroid hormone, synthetic progestin
B=prevents ovulation and may inhibit fertilization or implantation: Binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like levonorgestrel will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus
C= emergcency contraceptive(high dose) irregular cycle disorders (dose dependent), or in combination with other hormones as an oral contraceptive.
53
Lidocaine
```
A= class 1b antiarrhytmic, local (amide type) anaesthetics, Cardiac depressant
B= blocks activated and inactivated sodium channels with rapid kinetics, depresses ventricular excitability and the stimulation threshold for ventricular is increased during diastole (shortens repolarization and slows the depolarization process by acting in stage 4 of AP)
C= arrhytmias, termination of ventricular tachycardia/ arrhytmias, prevention of afib
Local/regional anaesthesia (= surface anaesthesia, infiltration anaesthesia, spinal/lumbar anaesthesia, epidural block)
```
54
Loratadine
```
A= antihistamine, pharmacodynamic antagonist, specific competetive h1 blocker - 2nd generation
B= competetive antagonist/inverse agonist at H1 receptors:⬇️tone of bronchial SMC, ⬇️️GIT tone, ⬇️venous blood vessel tone and vascular permeability and edema,⬆️ tone of arterial bv⬇️ effects of CNS (no nausea or vomiting)
C= nasal allergies, seasonal rhinitis (hay fever) treatment and prevention of urticaria, pruritis, insect bites and sting, food and drug allergy, nausea and vomiting, occasional insomnia
```
55
Lornoxicam
```
A= NSAID, oxicam group
B= inhibits both COX1 and COX2 (more selective to COX2) --> inhibits prostaglandin synthesis from arachidonic acid. (Does not lead to an increase in leukotriene formation --> reduces risk of adverse reactions unlike other NSAIDS)
C= osteoarthritis, rheumatoid arthritis, used as a painkiller e.g. in pain induced by dysmenorrhea, ocular inflammation, ankylosing spondylitis, keratosis, acute gout, postoperative pain, poly arthritis, fibromyalgias, arthrosis
```
56
Magnesium sulfate
A= anticonvulsant, replacement therapy
B=hypermagnesemia may depress the CNS and block peripheral neuromuscular transmission producing anticonvulsant effects. The excess magnesium appears to decrease the amount of ach and slows the rate of SA node
C= preeclampsia, eclampsia, prevention and control of seizures, acute nephritis in children, treatment and prevention of hypomagnesia, life threatening arrhytmias (?)
57
Memantine
```
A= neuroprotector, noncompetetive NMDA receptor antagonist.
B= blocks NMDA receptors and thus inhibits glutamate release which is toxic in large amounts. Also blocks influx of Na+ and Ca2+ but permitting sufficient influx of these ions to maintain vital processes
C= dementia, vascular dementia, alzheimers(!)
```
58
Mesalazine (?)
A= NSAID, 5-ASA containing agent (aminosalicylates)
B= mucosal production through arachidonic acid metabolites (both though COX, i.e prostanoids, pathway and lipoxygenase pathways, I.e. Leukotrienes, s increased in patients with IBS. Mesalazine diminish the inflammation by blocking COX and inhibiting production of prostaglandins.
(Katzungs: Other potential mechanisms of action of the 5-ASA drugs relate to their ability to interfere with the production of inflammatory cytokines. 5-ASA inhibits the activity of nuclear factor-κB (NF-κB), an important transcription factor for proinflammatory cytokines. 5-ASA may also inhibit cellular functions of natural killer cells, mucosal lymphocytes, and macrophages, and it may scavenge reactive oxygen metabolites.)
C= !IBD treatment! (ulcerative colitis and chrons disease)
59
Metformin
```
A= first line biguanides, antihyperglycemic drug
B= reduces hepatic and renal gluconeogenesis (through activation of AMP-activated protein kinase) and thereby decreases endogenous glucose production, also slows glu absorption from gut and increases sensitivity against insulin
C= DM2, Polycystic ovarian syndrome
```
60
Methotrexate
```
A= synthetic antimetabolite, immunosuppressant, first line non biologic DMARD
B= at low doses inhibits aminoimidazolecarboxamide ribonucleotide tranaformylase (AICAR) and thymidylate synthetase. They are normally required for the inhibition of AMP deaminase --> i/c levels of AMP increases which is then released and converted to adenosine which is a potent inflammatory inhibitor. As a result inflammatory functions of neutrophils, mphs, dendritic cells and lymphocytes are suppressed. Methotreate also directly inhibits proliferation and stimulates apoptosis in inflammatory cells + inhibits folic acid synthetase --> inhibit production of tetrahydrofolic acid which is required for DNA synthesis (high doses)
C= RA, SLE, juvenile chronic arthritis, ankylosing spondylitis, polymyositis, dermatomyositis, Wegners granulomatosis, giant cell arteritis, vasculitis
```
61
Methylprednisolone
```
A= glucocorticoid
B= binds to i/c nuclear glucocorticoid receptors --> the ligand bound receptor complex then moves to the nucleus where it interacts with the DNA and nuclear proteins by binding to the GRE at the promoter regions of responsive genes --> regulating the genes and thus the protein synthesis. The anti-inflammatory properties are thanks to lipocortins (phospholipase A2 inhibitory proteins) which controls the biosynthesis of prostaglandins and leukotrienes through the inhibition of arachidonic acid. Specifically induce lipocortin-1 synthesis which then binds to cell membranes, preventing phospholipase A2 from coming in contact with its substrate arachidonic acid--> diminished production of prostaglandins and eicosanoids. The COX1 and COX2 enzymes are also suppressed. Additionally, the immune system is suppressed by corticosteroids due to a decrease in the function of lymphatic system, a reduction in immunoglobulin & complement concentrations and the interference with antigen-antibody binding
C= for the relief of inflammatory dermatoses, endocrine disorders (adrenal insufficiency, addis ins disease), immune and allergic diseases, arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, chrons disease, collagen diseases, some neoplastic conditions, RA, acute leukaemia
C= maintenance treatment of asthma, allergic rhinitis (seasonal or prerennial). Chrons disease GvHD
```
62
Metoprolol
```
A= adrenonegative drug, selective beta1 antagonist without ISA
B= blocks beta1>beta2 (cardioselective) --> reduces cardiac output (negative ino/batmo/chrono/dromotropic effects)
C= angina pectoris, hypertension, arrhythmias, migraine, stenocardia, acute myocardial infarction, chronic heart failure!
```
63
Midazolam
A= benzodiazepines, short acting, Sedative – hypnotic agent
B= binds to specific GABAa recepors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening --> enhancing membrane hyperpolarization --> sedation and relief of anxiety, amnesia, hypnosis, anaesthesia, coma and resp depression (dose dependent depressant of CNS)
C=used for insomnia, seizures&epilepsy, relief of anxiety, for sedation and amnesia before and during surgery, as a component of combined anesthesia, for muscle, premedication(!)
64
Montelukast
```
A= leuktriene receptor antagonist,
B= blocks the action of leuktriene D4 on the cysteinyl leukotriene receptor CysL T1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by leuktrienes, and results in less inflammation
C= asthma treatment (not acute episodes) allergic rhinitis, obstructive lung diseases
```
65
Morphine
A= phenanthrene opioid agonist, analgesic, sedative agent
B= binding to and activating the μ-opioid receptors in the
central nervous system. Activation of the μ-opioid receptors is associated with analgesia,
sedation, euphoria, physical dependence and respiratory depression. (by agonizing the receptor the opioid close voltage gated ca2+ channels on presynaptic neurons--> reduce transmitter release as well as hyperpolarize and thus inhibit postsynaptic neurons by opening K+ channels)
C= cough in terminal disease, acute pain, severe pain premedication, postoperative pain, myocardial infarction, acute pulmonary oedema, chronic severe pain in palliative care, adjunct to rehydratation in acute diarrhoea.
66
Nebivolol
```
A= adrenonegative drug, cardioselective beta1 antagonist without ISA, class 2 antiarrhytmic
B= blocks beta 1 receptors + increased production of NO (further vasodilation, ERF) --> lowers heart rate and pressure. Also prevents release of renin. At high conc it may bind to beta2 receptors
C= angina pectoris, hypertension, arrhythmias (SV/V)
```
67
Nifedipine
```
A= calcium channel blocker, 2nd generation dihydropyridine derivative, vasoselective
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) may also facilitate the release of kidney stones
C= hypertension, angina pectoris, anti arrhythmiac, prinzmetal angina
```
68
Omeprazol
```
A= irriverisble PPI, antisecretory
B= inhibit gastric acid by blocking the H+/K+ATPase enzyme system (proton pump) of the gastric parietal cell of the fundus--> release of hydrogen is Inhibited and thus blocks the final step in acid production
C= gastric and duodenal ulcers, in combination with antibiotics for eradication of Hpylori infection, GERD, zollinger-ellison syndrome
```
69
Ondansetron
```
A= specific competetive 5HT3 serotonin antagonist, antiemetics
B= 5HT3 receptor blockade in gut, extrinsic intestinal Vagal nerves and afferent spinal neves, and CNS(vomiting center). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
C= prevention of nausea and vomiting associated with surgery, chemotherapy and anesthetics
```
70
Oxytocin
```
A= posterior pituitary hormone
B= stimulates SMC to facilitate ejection of breast milk (cause contraction of myoepithelial cells) and induces uterine contractions. Oxytocin acts through Gprotein coupled receptors and the phosphoinositide-calcium 2nd messenger system to promote uterine contractions. Also stimulates the releae of PGs and leuktrienes.
C= post-partum hemorrhage, induction of labor for e.g. medical reasons or in hypotonic uterine inertia, misscarriage treatment
```
71
Pancreatin
```
A= pancreatic enzyme preparation
B= contains replacement enzymes from animal pancreatic extracts (lipase, amylase, protease) --> improves digestion of dietary fat, protein and carbohydrates
C= replacement therapy for patients with deficient pancreatic exocrine function, chronic pancreatitis, CF
```
72
Paracetamol (us: acetaminophen)
```
A= non-opioid analgesic, antipyretic
B= inhibits COX-1 and COX-2 enzymes in peripheral tissues (without anti-inflammatory properties). COX normally converts the fatty acid arachidonic acid into endoperoxidase, prostaglandins and thromboxanes.
C= treatment of mild to moderate pain: headaches, myalgias, postpartum pain, postop pain, tooth aches, menstruation induced pain, fever
```
73
Paroxetine
```
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
```
74
Perindopril
```
A= antihypertensive drug, ACE inhibitor
B= acts by blocking the ACE that normally hydrolyes angiotensin I to angiotensin II and inactivates bradykinin (plasma kininase). this leads to decreased amount of angiotensin II and increased amount of bradykinin(vasodilator) -->vasodilation and inhibition of aldosterone secretion (reduces peripheral vascular resistance and decreases sodium and water retention) --> decreases bp
C= Hypertension, heart failure, myocardial infarction, left ventricular dysfunction, diabetic nephropathy, renal protector
```
75
Physostigmine (neostigmine)
```
A= cholinopositive drug, indirect acting parasympathomimetics, reversible anticholinesterase (carbamate + modest direct acting property; activates nicotinic receptors too)
B= blocks enzymes cholinersterases (ACHE and butyrylcholinesterase) by forming covalent bonds with them --> evokes prolonged effects of acetylcholine in the synaptic cleft--> stimulates N and M receptors through the activity of ACE
C= glaucoma(physostigmine), myasthenia gravis(improves muscle tone), decurarization (reversal of anticholinergic effects), muscle paralysis, atony of guts and bladder, central paralysis
```
76
Piracetam
A= nootropic/memory enhancer, GABA mimetics
B=influences neuronal and vascular functions and influences cognitive function without acting as a sedative or stimulanT. Also acts as an allosteric modulator of the AMPA receptor. It is hypothesized to act on ion channels or ion carriers; thus leading to increased neuron excitability. Improves the function of the neurotransmitter acetylcholine via muscarinic cholinergic (ACh) receptors, which are implicated in memory processes. May have an effect on NMDA glutamate receptors, which are involved with learning and memory processes
C= cognitive impairement, e.g. after strokes, dementia, cirulation disorders, Alzheimers
77
Prednisolone
```
A= glucocorticoid
B= binds to i/c nuclear glucocorticoid receptors --> the ligand bound receptor complex then moves to the nucleus where it interacts with the DNA and nuclear proteins by binding to the GRE at the promoter regions of responsive genes --> regulating the genes and thus the protein synthesis. The anti-inflammatory properties are thanks to lipocortins (phospholipase A2 inhibitory proteins) which controls the biosynthesis of prostaglandins and leukotrienes through the inhibition of arachidonic acid. Specifically induce lipocortin-1 synthesis which then binds to cell membranes, preventing phospholipase A2 from coming in contact with its substrate arachidonic acid--> diminished production of prostaglandins and eicosanoids. The COX1 and COX2 enzymes are also suppressed. Additionally, the immune system is suppressed by corticosteroids due to a decrease in the function of lymphatic system, a reduction in immunoglobulin & complement concentrations and the interference with antigen-antibody binding
C= for the relief of inflammatory dermatoses, endocrine disorders (adrenal insufficiency, addis ins disease), immune and allergic diseases, arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, chrons disease, collagen diseases, some neoplastic conditions, RA, acute leukaemia
C= maintenance treatment of asthma, allergic rhinitis (seasonal or prerennial). Chrons disease GvHD
```
78
Procainamide
```
A= class 1a antiarrhytmic drug
B= Ina and Ikr blockade--> by blocking sodium channels it slows the upstroke of f AP, slows conduction and prolongs Qrs. It also prolongs APD by nonspecific blockade of potassium channels--> prolongs refractory period
C= most atrial and supraventricular/ventricular arrhytmias, ventricular arrhytmias associated with acute myocardial infarction
```
79
Progesterone (dydrogesterone)
A= steroid hormone, orally active progestogen
B=Dydrogesterone is a progestogen that works by regulating the healthy growth and normal shedding of the womb lining by acting on progesterone receptors in the uterus.
C=Used to treat irregular duration of cycles and irregular occurrence and duration of periods caused by progesterone deficiency. absent, irregular or painful menstrual periods, infertility, premenstrual syndrome and endometriosis. Also used to prevent natural abortion in patients who have a history of habitual abortions.
80
Propranolol
```
A= adrenonegative drug, non cardioselective beta blocker without ISA, class 2 antiarrhytmic drug
B= blocks beta1and 2 receptors --> reduction in caricac ino-chronotropic-batmo-dromotropic effects as well as blood pressure and reflex orthostatic hypotension. Prevents sympathetic cardiac stimulation/ and reduce plasma renin secretions
C= angina pectoris, hypertension, tachycardia, heart failure, migraine, anti-anxiety activity (blocks serotonin receptors) acute myocardial infarction, hyperthyroidism, pheochromocytoma
```
81
Quetiapine
```
A= Newer antipsychotic preparation, atypical antipsychotic
B= a combination of antagonism at D2 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 (konst: 5-HT2 > D2 + 5HT1 partial agonist)
C= Schizophrenia, psychosis, bipolar disorders (manic phase), agitation in Alzheimers and Parkinsons, major depression disorder
```
82
Ranitidine
```
A= antihistamine, pharmacodynamic antagonist, specific competetive H2 blocker
B= competetive antagonist/inverse agonist at h2 receptors --> blocks effects of h2 receptors: ⬆️gastric secretion ⬇️ heart function and rhythm ⬆️ tone of arterial SMC bv ⬆️ womb contractions, increased release of granules of mast cells and basophils, decrease CNS effects of nausea and vomiting. Inhibits secretion of gastric acid mainly in two ways: 1) histamine released from ECL cells in stomach is blocked from binding to its receptors on parietal cells which stimulate acid secretion 2) other substances as gastrin and ach that stimulate acid secretion have a reduced effect on parietal cells when h2 receptors are blocked
C= gastric and duodenal ulcers, GERD, zollinger-Ellison disease, undiagnosed dyspepsia, healing of NSAID associated ulcers (specially duodenal)
```
83
Risperidone
```
A= Newer antipsychotic preparation, atypical antipsychotic
B= blocks 5HT2a receptors (inverse agonist) >D2 + 5-HT1 partial agonist-->modulating the release of dopa,NE, glut, GABA, ach and other neurotransmitters in the cortex, limbic region and striatum
C= Schizophrenia, psychosis, bipolar disorders (manic phase), agitation in Alzheimers and Parkinsons, major depression disorder
```
84
Rivaroxaban
A= oral anticoagulant, direct acting factor Xa inhibitor
B=Rivaroxaban competitively inhibits free and clot bound factor Xa. Inhibition of factor Xa interrups the intrinsic and extrinsic pathway of blood coagulation cascade, inhibiting both thrombin and formation and development of thrombi.
C= prevention of venous thromboembolism, thromboembolic prophylaxis in afib, pulmonary embolism, DVT, stroke prophylaxis
85
Rivastigmine
```
A= cholinopositive drug, indirect acting parasympathomimetics, selective ACE
B= blocks enzymes cholinesterases => amplifies endogenous conc of ach => increases cholinergic activity (cross blood-brain barrier)
C= Alzheimer's disease (improves cognitive functions but do not cure)
```
86
Rosuvastatin (atorvastatin)
```
A= statins
B= competetive inhibitor of HMG coA reductase -> reduced cholesterol synthesis and up regulate LDL receptors on hepatocytes --> 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) (Atherosclerotic vascular disease (primary and secondary prevention +acute coro- nary syndromes)
```
87
Salbutamol
```
A= adrenopositive drug drug, selective Beta2 receptor agonist
B= binds to and activates beta2 receptors mainly located on SMC of airways --> cause bronchodilatation. (Increases cAMP by activating adenylyl Cyclase, which increases activity of protein kinase A which inhibits phosphorylation of myosin and lowers I/c levels of ca2+.)
C= used as a bronchodilator in case of asthma or reversible airway obstructions, COPD, asthma prophylaxis
```
88
Sildenafil
```
A= vasoactive agent, vasodilator, PDE5 inhibitor
B= elevates i/c levels of the second messenger cGMP by inhibiting its breakdown through blockade of PDE5. Increased cGMP leads to vasodilation (blocks uptake of ca2+) which facilitates generation and maintenance of an erection
C= erectile dysfunction, pulmonary arterial hypertension
```
89
Spironolactone
```
A= synthetic steroid, aldosterone antagonist, potassium sparing diuretic, antihypertensive
B= blocks cytoplasmic mineralocorticoid aldosterone receptors in collecting tubules of nephrons --> increased salt and water excretion while potassium is retained. Also blocks androgen receptors--> anti androgenic effects
C= chronic heart failure, aldosteronism (conns syndrome, adrenal tumors), hypertension, edema in patients with congestive heart failure and nephrotic syndrome, hypokalemia,
```
90
Tamsulosin
```
A= adrenonegative drug, competitive uroselcetive alpha1 antagonist
B= has higher affinity for alpha1a and alpha1d receptors located on SMC of prostate and urinary bladder --> relaxes smc more than peripheral vessels
C= benign prostatic hyperplasia (not hypertension)
```
91
Tolterodine
```
A= cholinonegative drug, m3 selective competetive antagonist
B= blocks M3 and M2 receptors located on detrusor muscle of bladder -->inhibition of bladder contraction, decrease in detrusor pressure and an incomplete emptying of bladder
C= urinary incontinence
```
92
Torasemide
```
A= antihypertensie drugs, pyridine-sulfonylurea type loop diuretics
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= heart faiulre, severe hypertension, edemas, empathic cirrhosis, renal impairment, nephrotic syndrome, hypercalcemia
```
93
Trihexyphenidyl
```
A= cholinonegative drug (centrally and peripherally acting) selective m1 receptor antagonist
B= blocks cholinergic activity in CNS and increases availability of dopamin---> smoother control of voluntary muscle movement + corrects the relative cholinergic excess in basal ganglia
C= reduces sialorrhoea, tremor and ridgidity --->parkinsons disease treatment
```
94
Tropicamide
```
A= cholinonegative drug, muscarinic antagonist
B= binds to and blocks muscarinic receptors in eye muscles (mainly M4 receptors)--> blocks the responses of the iris sphincter muscle and ciliary muscles to cholinergic stimulation, producing dilation of pupil and paralysis of ciliary muscle
C= promotes mydriasis and cycloplegia for eye examinations
```
95
Ursodeoxycholic acid (ursodiol)
```
A= choletropic, choleretic agent, bile acid
B= promote producing and secretion of bile and also reduces the concentration of cholesterol in bile by reducing hepatic cholesterol secretion and inhibits intestinal absorption (--> dissolves gallstones)
C= gallstone treatment for patients not eligible for surgery
```
96
Valproic acid (valproate)
```
A= GABA mimetics, 1st line broadspectrum antiepileptic, antimanic/mood stabilizer¨
B= increases GABA levels in the brain by: 1) facilitating glutamic acid decarboxylase --> enzyme responsible for GABA synthesis 2) blocks the action of GABA transaminase --> blocks degradation of GABA. Also blocks NMDA-receptor mediated excitation ---> blocks sustained high-frequency repetetive firing of neurons
C= seizures, myoclonic seizures, tonic clonic seizures, bipolar disorders, migraine prophylaxis
```
97
Warfarin
A= indirect acting
oral anticoagulant, a coumarin derivative
B= interferes with the hepatic synthesis of vit K dependent coagulation factors II (prothrombin), VII (proconvertin), IX(christmas factor) and X (Stuart-prower factor). Antithrombogenic effect generally occurs only after factors X and IX are diminished (usuall 2-7 days after initiation of therapy. [blocks gamma-carboxylation of several glutamine residues in these coag factors+ protein C and S --> results in inactive incomplete coag factors
C= For the treatment of retinal vascular occlusion, pulmonary embolism, cardiomyopathy, atrial fibrillation and flutter, cerebral embolism, transient cerebral ischaemia, arterial embolism and thrombosis
98
Zolmitriptan
```
A= direct selective 5-HT ID/IB receptor agonist (ser receptors)
B= binds to and activates 5-HT ID/IB receptors on presynaptic trigeminal nerve endings to inhibit the release of vasodilating peptides thus preventing the stretching of stretch receptors and leading to cranial blood vessel constriction -->reducing headaches
C= acute episodes of migraine
```
99
Zolpidem
```
A= newer hypnotic drug, imidazopyridine derivative, BZ analog
B= binds to specific GABAa ω2 receptors (btw the alpha1 and gamma2 subunits in the pentameric receptor) in CNS neuronal synapses that facilitates the frequency of GABA-mediated opening of chloride ion channel opening --> enhancing membrane hyperpolarization --> sedation and relief of anxiety, amnesia, hypnosis, anaesthesia, coma and resp depression (dose dependent depressant of CNS)
C= sleeping disorders!
```
100
Aciclovir
```
A= antiviral drug, nucleoside analog
B= inhibits viral DNA polymerase --> inhibts nucleic acid synthesis + chain terminantion following incorporation into the viral DNA (prodrug, hydrolyzed to its active metabolite in the organism. Selectively metabolized= the active form only accumulates in infected cells)
C= Herpes simplex type 1 and 2, varicella-zoster, Epstein Barr virus
```
101
Amoxicillin/Clavulanic acid
```
A= 3rd generation penicillins; broad spectrum AMINOpenicillins, bactericidal drug / Beta lactamase inhibitor
B= inhibits bacterial CW synthesis by binding to PBPs thus blocking transpeptidation of the peptidoglycan ---> CW disrupts. Aminopenicillins have additional aminogroup which make them able to penetrate the O.M of gram- microbs. Clavulanic acid interferes with beta lactamase enzymes which allows amoxicillin to perform its function and therefore prevents the drug from being hydrolyzed by beta lactamases(drug synergism)
C= Gonococcal infections, upper RTI, uncomplicated UTi, and sinusitis & otitis media caused by susceptible organisms
```
102
Atovaquone/Proguanil
```
A= antimalarial drug, antiprotozoal
B= ato: disrupts the electron transport chain in the mitochondria. pro: inhibits dihydrofolate reductase -->inhibits folic acid synthesis --> inhibits DNA synthesis
C= treatment and prevention (chemoprophyslaxis) of malaria, mild to moderate P jiroveci pneumonia
```
103
Benzylpenicillin
```
A= beta lactam antibiotics, Natural penicillins, 1st generation
B= inhibits CW synthesis by blocking transpeptidation by binding to the active site of PBPs, thus inhibits the transpeptidation reaction & arrests peptidoglycan synthesis --> cell lysis (bacteriocidal)
C= streptococcal (incl pneumococcal), gonococcal and meningococcal infections and also for anthrax, diphtheria, gas-gangrene, leptospirosis, and treatment ofLyme disease in children (treponama pallidum and certain other spirochetes), Clostridium spp, actinomyces and certain other gram + rods and nonBetalactamase producing gram - anaerobs
```
104
Ceftriaxone
```
A= antibiotics, 3rd generation cephalosporins
B= inhibition of CW synthesis by inhibition of transpeptidase --> reducing CW stability --> cell lysis (bactericidal)
C= serious infections such as septicaemia, pneumonia and meningitis; Citrobacter, S. marcesens and Providencia infections + beta lactamase producing Haemophilus and Neisseria, pneumococci + surgical prophylaxis
```
105
Cephalexin
A= antibiotics, 1st generation cephalosporins (broad spectrum)
B=inhibition of CW synthesis by inhibition of transpeptidase --> reducing CW stability --> cell lysis (bactericidal)
C= gram-positive organisms (except enterococci), incl penicillinase producing staphylococci and strep infections, gram negative organisms such as E coli and K.pneumoniae :UTIs
106
Ciprofloxacin
```
A= fluoroquinolones
B= bactericidal activity against susceptible bacteria; inhibits DNA replication by bindint to DNA gyrase and topoisomerase IV
C= UTI, bacterial prostatitis, RTIs, bacterial diarrhoea, mycoplasmal infections, gonorrhoea, septicaemia, GIT infections (incl typhoid fever), bone and joint infections, non-gonococcal urethritis and cervicitis
```
107
Clarithromycin
```
A= Macrolide antibiotic, erythromycin derivative
B= inhibits bacterial protein synthesis by interfering with the 50s ribosomal subunit by lactone rings --> peptidyl -tRNA is dissociated from the ribosome
C= streptococcal infections, syphilis, RTI, mycoplasmal infections, Lyme Disease. First line treatment of H pylori. Mycobacterium avium complex+ mycobacterium leprae, toxoplasma gondii and H.influenzae
```
108
Clotrimazole
```
A= imidazole derivative, antifungal (azoles 1st generation)
B= reduces ergosterol synthesis by inhibition of fungal cytochrome P450 enzymes (lanesterol demethylase) --> disrupts CM synthesis and renders it leaky --> cell lysis and death
C= Candida spp (oral thrus, vulvovaginal candidiasis), C neoformans, mycoses, dermatophytes
```
109
Co-trimoxazole
A=synthetic antibiotics, a dihydrofolate reductase inhibitor (trimethoxybenzylpyrimidine) + a sulfonamide (sulfamethoxazole)
B= trimethoprim given together with the sulfonamide produce sequental blocking resulting in drug synergism of the activity of both drugs. Trimethoprim inhibits dihydrofolate reductase of bacteria, which blocks the conversion of dihydrofolic acid to tetrahydrofolic acid and subsequently blocks the synthesis of purines and DNA. Sulfamethaxozole, as a structural analog of PABA (part of folic acid) competes for the incorporation of this subunit into the folic acid --> inhibits folic acid synthesis
C= RTI, UTI, prostatitis, acute exacerbations of chronic bronchitits, acute otitis media and sinusitis, shigellosis and salmonella infections, Pneumocisa carinii pneumonia
110
Doxycyline
```
A= broad spectrum tetracycline antibiotic (bacteriostatic)
B= inhibits bacterial protein synthsis by binding to the 30S ribosomal subunit and prevents adding of a.a. to the growing peptide chain (reversibly)
C= syphilis, chlamydial infections, Lyme disease, mycoplasmal infections, acne, rickettsial infections, Brucella, acne, prophylaxis of travelers diarrhoea
```
111
Fluconazole
```
A= wide sprectrum antifungal, Triazole antifungal (azoles of 2nd generation)
B= blocks fungal P450 cytochrome enzymes and subsequently interferes with ergosterol synthesis
C= candidomycoses, systemic mycoses, tinea pedis/corporis/cruris/pitiriases versicolor and dermal candidiasis, (systemic and subcutaneous mycoses)
```
112
Isoniazid
```
A= first line synthetic antituberculous drug
B= Can penetrate into mphs and is therefore active against both intracellular and extracellular microbs. inhbits mycolic acid synthesis --->inhbits CW synthesis: by forming a complex with an acyl carrier protein and a beta-ketoacyl carrier protein synthetase which are normally required for mycolic acid synthesis
C= first line treatment of tuberculosis (+ latent tbe)
```
113
Itraconazole
```
A= wide sprectrum antifungal, Triazole antifungal (azoles of 2nd generation)
B= blocks fungal P450 cytochrome enzymes and subsequently interferes with ergosterol synthesis
C= dermatophytic (tinea) skin infections, pityriasis versicolor, histoplasmosis, systemic infections (aspergillosis, candidiasis, cryptococcosis) oral and vaginal candidiasis, onychomycosis. (Subcutaneous and systemic mycoses)
```
114
Mebendazole
A= wide spectrum antihelminthic (anti-worm) drugs, synthetic benzimidazole
B=inhibits microtuble synthesis of the parasites + decreases parasites glucose uptake
C= intestinal nematodiasis (roundworms), intestinal cestodiasis and trematodiasis (tapeworms and intestinal flukes) + ascariasis, trichuriasis, hookworm and pinworm infections
115
Metronidazole
```
A= synthetic 5- nitroimidazole antiprotozoal
B= M is selectively absorbed by anaerobic bacteria and susceptible protozoa, where it is nonenzymatically reduced by reacting with reduced ferredoxin. this reduction results in products that are toxic to anaerobic cells. The metabolites of metronidazole are taken up into bacterial DNA, forming unstable molecules.
C= acute invasive amoebic dysentery (entamoeba histolytica), anaerobic protozoa and anaerobic bacteria (Bacterioides and Clostridium), urogenital trichomoniasis, giardiasis, balantidiasis, bacterial vaginosis, anaerobic infections such as meningitis and peritonitis
```
116
Oseltamivir
```
A= antiviral, neuraminidase inhibitor, sialic acid analog
B= transition state analog inhibitor of NA, preventing progeny virions from emerging from infected cells (prodrug). (Inhibition of viral NA results in clumping of newly released influenza virions to each other and to the membrane of the infected cell)
C= treatment and prophylaxis of inflenza type A and B + respiratory syncytial virus
```
117
Permethrin
A= antiparastitic, ectoparasiticide
B=acts on the nerve cell membrane to disrupt the sodium channel current by which the polarization of the membrane is regulated. Delayed repolarization and paralysis of the pests are the consequences of this disturbance.
C= Pediculus humanus, Pthirus pubis and Sarcoptes scabiei infections (pediculosis, scabies) (pest control in agriculture, households and industries)
118
Terbafine
A= allylamine antifungal drug
B=Selectively inhibits the epoxidation of squalene, thus blocking the syntheis of ergosterol -->disrupt fungal CM
C= onychomycosis and dermatophytosis
119
Rifampicin
A=first line antituberculous antibiotic. semisynthetic
B= binds to the beta subunit of bacterial DNA-dependent RNA polymerase and thereby inhibits RNA synthesis
C= Mycobacterium infections, incl tbe and leprosy. MRSA infectios in combination with fusidic acid, H.influenzae type B prophylaxis in children
120
Povidone/Iodine
```
A= iodophors (complex of iodine with a surface active agent) antiseptics from halogens group
B= idodine is released and precipitates microbial proteins by forming salts as well as kills bacterial spores (sporocidal and bactericidal)
C= skin disinfectant for preoperative skin preparation or used as antiseptic. Able to kill vegetative bacteria, mycobacteria, fungi and lipid-containing viruses
```
Pharma Exam
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