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PBL year 2 (Sam) > Drugs > Flashcards

Drugs Flashcards

1
Q

Aluminium hydroxide

A

INDICATION:For relief of heartburn and acid indigestion

MOA:basic inorganic salt that neutralises HCl in gastric secretions to form Aluminium chloride and water

inhibits the action of pepsin by increasing pH

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2
Q

example of TNFa inhibitor

A

adalimumab- stop pro inflam action so no fever, activation of endothelium

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3
Q

pryidoxine

A

prophylaxis for isoniazid TB peripheral neuropathy

ligand for phyridoxal kinase

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4
Q

valsartan

A

treatment of hypertension to reduce risk of CV disasters + HF

Angiotensin receptor blocker-

selectively binds to AT1 and prevents ang II exerting its hypertensive effects (aldosterone and ADH production, cardiac stimulation, increased renal absorption of sodium)

by blocking AT1 you prevent downstream negative feedback RAAS activation (chronic assocaitation in HF)

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5
Q

gliclazide

A

INDICATION: sulfonylurea to treat hyperglycaemia in patients w T2DM

MECHANISM:

  • binds to B cell sulfonyl urea receptor
  • thus subsequently blocking the ATP sensitive potassium channels
  • decrease in K+ efflux
  • depolarisation of cell
  • opens voltage gated Ca2+ channels
  • calmodulin activation
  • exocytosis of insulin
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6
Q

alteplase

A

thrombolytic

1* target plasminogen

activator

2* target fibrinogen alpha chain

binds to fibrin rich clots via fibronectin kringle 2 domain

the protease domain cleaces the arg/ val bonds in plasmin

plsmin casues degradatoin of fibrin matric

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7
Q

efavirenz

Non-nucleoside reverse transcriptase inhibitor

Believed inhibition reverse transcriptase interferes with generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes then eliminate HIV particle that previously had been uncoated and left unprotected, during entry into host cells.

A
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8
Q

Clarithromycin

A

INDICATION: treatment of many infections- otitis media, H pylori influenza

macrolide

MOA: metabolised

penetrates bacterial cell wall and reversibly binds to the 23S and 50S subunits of the bacterial ribosome, blocking translocation of tRNA and polypeptide synthesis

stops action of P-glycoprotein a drug efflux pump

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9
Q

norepinephrine

A

precursor of epinephrine that is secreted by adrenal medulla and acts as a central autonomic NT

used as a vasopressor in shock situations- e.g, septic

acts on B1- inotropic effect— increased contractility and hr

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10
Q

trimethoprim

A

antibacterial (mainly gram positive) , antifolate, antiprotozoal

1* target- dihydrofolate reductase (bacterial)

reversible inhibitor (antagonist)

2* target- human dihydrofolate reductase

folate metabolism:

can’t form tetrahydrofolic acid —- can’t produce bacterial nucleic acids

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11
Q

omalizumab

A

Monoclonal antibody against human IgE

MOA:

  • binds to IgE w higher afinity than the Fc epsilonRI receptor on the surface of mast cells and basophils
  • this decreases the availability of free IgE for binding and to trigger the allergic cascade
  • reduction in surface bound IgE on FcERI cells limits the degree of release of inflam mediators e.g., Il4, Il5 and Il13
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12
Q

Metformin

A

INDICATION: adjunct to exercise and diet control in T2DM patients

MOA: taken up into hepatocytes

positively charged so accumulates in mitochondria

inhibits mitochondrial complex 1

prevents production of ATP

activates AMPK- important in glucose metabolism

inhibits gluconeogenesis and adenylate cyclase

ampk inhibits fat synthesis- reduces hepatic lipid stores, increase liver sensitivity to insulin

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13
Q

Amoxicillin

A

INDICATION:

Amoxicillin alone is indicated to treat susceptible bacterial infections of the ear, nose, throat, genitourinary tract, skin, skin structure, and lower respiratory tract.

Used in combo with clarithromycin to treat H. pylori infections.

MOA:

competitively inhibits penicillin-binding protein 1 and other high molecular weight PBPs

PBPs are responsible for glycosyltransferase and transpeptidase reactions that lead to cross-linking of D-alanine and D-aspartic acid in bacterial cell walls.

Without the action of penicillin binding proteins, bacteria upregulate autolytic enzymes and are unable to build and repair the cell wall, leading to bacteriocidal action

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14
Q

Hydroxychloroquine

A

INDICATION: acute RA, Chronic Ra, prophylaxis for malaria

Accumulates in cells and raises the pH

inhibits antigen processing by preventing the alpha and beta chains of the MHC II dimerisation

thereby inhibits APresentation of cell

self peptides bind to MHC with low affinity anyway so this decreases chances even more

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15
Q

Baclofen

A

INDICATION:

relexant for painful muscle spasms, antispastic agent especialluy against flexor compartment

parkinsons, cerbral palsy, stroke

MOA: depresses synaptic reflex transmission by stimulation of GABA- B receptors

inhibition of excitatory NT release (glutamate and aspartate)

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16
Q

Tenofivir

A

antiretroviral drug- nucleotide analogue reverse transcriptase inhibitor

tenofovir is absorbed and converted into its active form (nucelotide analgue)

tenofovir diphosphate inhibits HIV-1 reverse transcriptase by direct binding with the natural substrate

after integration into DNA it causes viral DNA chain termination

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17
Q

clopidogrel

A

antiplatelet antithrombotic

irreversibly inhibits ADP mediated platelet activation and interfering with GPIIb/IIIa aggregation

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18
Q

methotrexate

A

INDICATIONS: idiopathic joint pain, brain effusion, cancer

MOA: Methotrexate enters tissues and is converted to a methotrexate polyglutamate by folylpolyglutamate. inhibition of enzymes responsible for nucleotide synthesis including dihydrofolate reductase

In rheumatoid arthritis- accumulation of adenosine triphosphate and adenosine in the extracellular space, stimulating adenosine receptors, leading to anti-inflammatory action.

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19
Q

dabigatran

A

NOAC

inhibitor of thrombin stimulated platelet aggregation

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20
Q

Budosenide

A

corticosteroid—- asthma, ulcerative colitis

lipid soluble so they diffuse through the plasma membranes of cells and into the nucleus

where they bind to positive and negative glucocorticoid receptors

positive GREs increase anti inflam mediator expression (transactivation)

negative GREs reduce inflam expression (transrepression)

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21
Q

lactulose

A

treat acute onset hepatic encephalopathy assocaited with alcohol related liver disease

non curative but improves mental status

MOA:

nonabsorbale synthetic disaccharide that is broken down by sacchorolytic bacteria in the large intestines into organic fatty acids

high transient acid content in the gut draws nitrogenous bases from the blood

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22
Q

Gentamycin

A

braod spectrum aminogylcoside antibiotic used mainly on gram negatives

made of gentamycins C1, C2 and C1a

bind to ribosomal 30S subunit, casuding misreading of tRNA leaving the bacterium unable to synthesise new proteins needed for growth, survival and replication

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23
Q

trastuzumab

A

recombinant IgG1 kappa humanised monoclonal antibody

used to treat cancers positive for HER2 (human epidermal growth factor receptor)

binds to the extracellular ligand binding domain and blocks the cleavage of HER-2 to induce its receptor downmodulation. Inhibition of MAPK and P13K/Akt parhways lead to an increase in cell cycle arrest, suppression of cell growth and proliferation.

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24
Q

atorvastatin

A

INDICATION: antilipodaemic

MOA: reversibly competitively inhibits HMG-CoA reductase

HMG reductase is rate limiting step in cholesteropl synthesis

decreases hepatic cholesterol concs, stimulating the upregulation of LDL receptors–> increases LDL uptake

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25
Emtricitabine
nucleoside reverse transcriptase inhibitor gets phosphorylated competes with normal HIV reverse transcriptase gets integrated into DNA and terminates new chain formation .
26
phentolamine
Antihypertensive 1\* target-- A1 receptor (GPCR) effect- partial antagonist causes vasodilation usually 2\* target- B1 receptor (GPCR) effect- agonist stimulates positive inotropic effect
27
Bisoprolol
B blocker stops inotropic effects of B1 receptors
28
Esomeprazole
INDICATION: PPI used in acid refluc disorders, pewptic ulcer diease and H pylori infection, NSAID abuse MOA: prevents final step in HCl production by covalently binding to sylfhydral group found on H+K+-ATPase enzyme at the secretory surface of gastric parietal cells. Limits secretion of HCL
29
antiretroviral medication examples brief
nucleoside reverse transcriptase inhibitors- inhinit dna synthesis via reverse transcriptase and act as DNA chain terminators protease inhibitors- compeitive inhibnition of HIV aspartyl protease- used to produce functional viral proteins integrase inhibitors fusion inhinitors
30
doxycylin
borad spectrum antibiotic used to treat gram positive and negative bacteria e.g., mycoplasma pneumoniae mainly bacteriostatic (keep in stationary phase) * target 30S prokaryotic ribosomal unit during protein synthesis * prevents binding of tRNA and mRNA at the ribosomal subunit * therefore no amino acids can be added to the polypeptide chain * no new proteins
31
glyceryl trinitrate
Vasodilator so heart doesnt work as hard 1\* target= mitochondrial aldehyde dehydrogenase activity- produces more NO 2\*target- guanylate cyclase agonist-- more cGMP- more PKG- more myosin phosphatase- relaxation of sm muscle
32
Amlodipine and atropine
antihypertensive L- type calcium channel antagonist inhibiting influx into vascular smooth muscle and cardaic muscle less Ca2+/ calmodulin less MLCK activation more MLC-P activation less sm muscle contraction less vasoconstriction- lower blood pressure stronger effect on smooth muscle e.g., than cardiac
33
Ramipril
INDICATION: mild to severe hypertension (associated w T2DM) MOA: ACE inhibitor inactive prodrug converted to ramiprilat in the liver anatgonises RAAS by competitive inhibition EFFECTS: decreased production of AT-II therefore less vasoconstriction and less release of aldosterone and less break down of bradykinin (dilator)
34
Magnesium triscillate Mg2O8Si3
INDICATION: antacid for peptic ulcers and releaving heartburn H.PYLORI BARRET'S MOA: gelatinous silicon dioxide formed in a neutralisation reaction with H+ of Hcl is protective and favours healing often prescribed w alumimium as mag has a longer lasting effect
35
location and action of a1 receptor B1 B2 Dopaminergic
a1 peripheral, renal and coronary circulation------ vasoconstriction B1- heart---- increase contractility and HR B2- lungs, periphery and coronary circulation----- vasodilation and bronchodilation dopaminergic- mesneetric, renal and coronary arteries------ vasodilation
36
warfarin
anticoag inhibits reduction of vitamin k prevents y-carboxylation of glutamate residues in factors II, VII, IX and X
37
groups of antihypertensives
diuretics ACE inhibs ANG II converting blockers Direct renin inhibitors Beta blockers calcioum channel blockers alpha blockers central agonists
38
prednisolone
glucocorticoid similar to cortisol INDICATION: ANTIINFLAMMATORY -- asthma relief MOA: inhinbits neutrophil apoptosis inhibits phospholipase A2 which decreases the formation of arachidonic derivatives- prostaglandins and thromboxanes **inhibit production of pro-inflams** as they bind to intracellular glucocorticoid receptor and then translocate to nucleus to act as TFs
39
carbimazole
antithyroid agent----- hyperthyroidism part of blocking regime with levothyroxine MOIA: decreases the uptake and concentration of inorganic iodine by thyroid, it also reduces the formation of di-iodotyrosine and thyroxine. Once converted to its active from of methimazole, it **prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine** residues on t**hyroglobulin**, hence reducing the production of the thyroid hormone T3 and T4
40
salbutamol
symptomatic relief and prevention of bronchospasm caused by asthma, bronchitis (obstrucitve) targets= B2 adrenoreceptor partial agonist analgoue of adrenaline B2R's present in smooth muscle cells and mast cells Gas pathway-- increase adenylylcylase -- increase 2nd messenger camp-- increased PKA and decreased calcium in cells-- deactivate MLC kinase and activate MLC-P-- decreased sm muscle contraction in bronchioles induces opening of K+ channels inducing hyperpolarisation
41
atropine
antimuscarinic (m3 inhib acetylcholine)- eye dilator and vasodilator competitive antagonist long lasting causes contraction of radial muscles in eyes----- **mydriasis** **M3= G**q-- **increase PLCB-**- **increase (IP3)**-- **increase {Ca2+}i**-- **contraction** m3 also found in vascular smooth muscle
42
Morphine
Indication: ANALGESIA, SEDATIVE MOA: acts on u opiod receptrors in the brain and spinal cord to inhibit pain transmission and modify the central perception of pain. opioid receptors are GPCRs which inhibit adenylate cyclase, open k+ channels and inhibit Ca2+ channel opening, thus desensitising nerve endings and requiring larger stimuli to trigger depolarisation
43
mepolizumab
**monoclonal antibody against Il5** **IL5 receptor activation stimulates differentiation of leukocyte progenitor cells**: * **Eosinophils** proloferate and migrate into tissues in response to Il5--- they secrete things like MMPs, TGFB,NO and ROS * primary cytokine associated w maturation, activation and prolonged survivial of **inflammatory neutrophils**
44
ferrous sulphate tablets
INDICATION: treat and prevent anaemia MOA: transported by DMT1 into macrophage incorporated into ferritin and stored eventually oxidised
45
isoniazid
antibacterial agent (bactericidal) used priamrily in TB prodrug that is activated by bacterial catalase inhibits production of mycolic acids
46
rivaro**_x_**aban
* anticoagulant * competitive inhibitor of FX * therefore inhibits the activation of FII * thrombin can therefore not convert fibrinogen to fibrin to secure the primary haemostatic plug of aggregated platelets
47
treating RA initial treatment ? \>? ?
initial- treat to target with cDMARD- corticosteroid and NSAID step up with bDMARD (biologic)- try TNFa inhibitors ritixumab- b cell modifier Il-6 inhibitors
48
Bismuth subsalicylate
Anti-diarrhoeal antisecretory action for water and ions in the intestines binds toxins made by E.coli
49
a calcidol
INIDCATION: hypothyroidism and rickets +T2DM bone weakness associated w kidney problems form of vit D used to regulate calcium and phsophate MOA: liver catalyses activation now activated, binds to intracellular receptors that act as TFs increase GI absorption of Ca and phosphorus increase osteoclastic resorption increasing renal absorption of calcium
50
Naproxen
inhibition of COX 1 and 2 enzymes ## Footnote 2- involved in convversion of arachidonic acid to prostaglandins that: sensitise nerve endings, potentiate vasodilators, mediate thermoregulatory response cox-1: pyhysiological gastro-protective effects regulate renal blood flow
51
co-careldopa
dopaminergic medicine as symptomatic relief in PD contains levodopa and carbidopa levodopa is a dopamine precursor which crosses the BBB before being converted into dopamine Carbidopa- is a peripheral DOPA-decarboxylase inhinbitor which prevents levodopa from being broken down in areas other than the brain
52
furosemide
INDICATION: potent loop diuretic used in ascites , CHF, hypertension MOA: blocking tubular reabsorption of sodium and chlride in the P and DCT Compeitive inhinition of NKCC2 (sodium- potassium- chloride transporters), prevents transport of Na+ from luminal to basolateral side for reabsorption. More less NaCl- detected by macula densa- activate RAAS
53
Sildenafil
decreases **pulmonary hypertension** via **vasodilation** **selective phosphodiesterase 5 inhibitor** **NO activates guanylate cyclase** **increased cGMP** which **activates PKG** which activates **myosin phosphatase** which dephosphorylates light chain of myosin II relaxation **PDE5** present in sm muscle of vessels **it usually degrades cGMP**
54
diazepam
INDICATION: benzodiazepine used as an anticonvulsant, anxiolytic and muscle relaxant in trmor, alcohol withdrawal, upper motor neurone disorders such as **cerebral palsy** **MOA:** act centrally binding to receptors in the brain. increases inhinbitory effect of GABA
55
picolax
soidum picosulphate--\> picosulfurinc acid treat constipation or induce colon cleansing to prepare large bowels for colonoscopy or surgery MOA: inhibits the absorption of water and elctrolytes and increases their secretion into the intestinal lumen. It is hydrolysed by colonic bacteria enzyme sulfatase to form the active metabolite which acts direcvtly on colonic mucosa to simtulate peristalsis
56
atenolol
B blocker non selective- block catecholamines from activating B1 (inotropic- contractility and HR) decreases renin releae and decreases sympathetic action
57
rifamipcin
treating tuberculosis 1\* target- DNA directed RNA polymerase subunit inhibitor leads to suprpession of RNA synthesis and cell death
58
low molecular weight heparin
binds reversibly to antithrombin III changing it to its active form and forming a complex together increases the rate at which ATIII inhibits IIa and Xa also inhibits IX, XI, XII and XIII shorter than natural heparin so have a shorter IIa length
59
sulfalazine
INDICATION: crohns and RA ?????? anti inflam properties high affinity for CT
60
Propanolol
INDICATION: thyrotoxicosis, hypertension ACTIONS: antidysrhtmic, antihypertensive, antianginal MOA: blocks actions of catecholamines (adrenaline) on B-adrenoceptors thereby blocking sympathetic drive, reducing pacemaker activity and increasing AV conduction time. Reduces slow inward tCa2+ gate opening during phase 4 (slow depolarisation)
61
Hydroxycobalmin (Vitamin B12)
INDICATION: vit B12 deficiency MOA: ?????
62
Loperamide
laxative, colonic cleansing inhibits peristaltic activity by being non-selective calcium channel blockers and binding to opoid U receptors. Inhinits epristalsis pf circular and longitudinal muscles
63
Sacubitril
**_INDICATION:_** used in combo with valsartan as **antihypertensives**, CHF 1\* TARGET= nephrilysin enzyme ACTIVITY= competitive inhibitor Neprilysin is a natural endopeptidase that cleaves and degrades natriuretic peptides (ANP, BNP and CNP) NP's are released in response to atrial and ventricular stretching, they activate downstream receptors leading to vasodilation along with sodium and water excretion. breaks down vasodilators and vasocosntrictors like ANg II therefore used in combo w valsartan to block ANGII receptors-- further no constriction

PBL year 2 (Sam) (12 decks)

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