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Year 2 > Unit 3/4 Drugs > Flashcards

Unit 3/4 Drugs Flashcards

1
Q

NAPROXEN

A

NSAID - LUPUS
Non-selective inhibitor of cyclooxygenase, an enzyme invovled in prostaglandin synthesis via the arachidonic acid pathway
Decreases the synthesis of prostaglandins involved in mediating inflammation, sensitizing nociceptors involved in transmitting pain, fever and swelling
Decrease in TXA2 so lack of platelet activation, adherence, aggregation

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2
Q

Folic acid

A

Heamolytic anemia

Folic acid= biologically inactive
converted to tetrahydrofolic acid-> methytetrahydrofolate from DIHYDROFOLATE REDUCTASE.

Transpoted across cells via endocytosis + synthesixe nucleic acids and hep erythropoesis

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3
Q

What type of drug is ivacaftor when is it indicated

A

Quinolone used treat CF

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4
Q

Side effects ivocaftor

A

Abdo pain + diarrhoea

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5
Q

MofA ivacaftor

A

G551D CFTR mutation - CFTR protein reach epithelial cell surface, but doesn’t let it transport chloride through the ion channel.

Ivacaftor = potentiator of the CFTR protein.

Ivacaftor facilitates increased chloride transport by potentiating the channel-open probability (or gating) of the G551D-CFTR protein.

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6
Q

What are the modulator drugs in CF used in triple therapy

A

Ivacaftor - potentiator of CFTR ion channel

tezacaftor is a CFTR corrector that moves the mutated CFTR protein to the correct place on the epithelial cell surface membrane

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7
Q

Other triple therapy drugs CF

A

Mycophenolate - inhibts IMPDH altering DNA formation - inhibiting proliferation t/b lymphocytes + supress AB formation

Tacrolimus - binds FKBP-12 therfore inhibitng t lymphocyte activation

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8
Q

Predisalone mofa

A

Glucocorticoid R agonist. Binds GR R - translocate nucleus binding GRE in promoter region in target gene. DNA bound R interacts TF to cause up/down reg specific target gene.

Anti inflam - phosphorylates + release annexin 1 - INHIBIT LEUKOCYTE TRAFFICKING

Supression AA
Depress macro function
Th1- Th2 responce

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9
Q

Belimumab mofa

A

Binds BAFF (over expressed SLE) * BAFF cant bind B cells * no longer survival or proliferative signal. Decrease B cell survival/ B cell mediated immunity

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10
Q

Rituximab mofa

A

Human monoclonal Ab against CD20 antigen found surface normal mature + malignant b lymphocytes. AB igG1 kappa IG leads selective lysis b cells * decreased b cell survival + b mediated immunity.

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11
Q

Drugs used in lupus

A

Predisalone
Belimumab
Rituximab

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12
Q

Tocilizumab

A

anti il-6 disrupting Th17 cells

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13
Q

Infliximab

A

Anti TNF alpha

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14
Q

drugs used triple therapy after bilateral lung transplant

A

prednislone
mycophenolate mofetil
tacrolimus

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15
Q

Oral flucox

A

Staph aureus found nasal passages + skin 15-40% healthy adults. Gram positive responsible MRSA/ MSSA. Start CF diagnosis long term AB for prophylaxis against staph aureus.

Narrow spec penicillin, beta lactam. Binds + inactivates PBP on inner cell membrane of bacterial wall. Inactivated PBP interferes cross linkage of peptidoglycan chains necc bacterial cell wall strength + rigidity. Interrupts bacterial cell wall synthesis * weakening wall + lysis.

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16
Q

IV vancomycin

A

Selective resistant strains gram +ve bacteria (staph aureous). Second line treatment failed respond oral AB

Glycopeptide. Binds to NAG/ NAM of synthesizing peptidoglycan preventing transpeptidase acting on these newly formed blocks * preventing cross linking peptidoglycan layer * layer more permeable/ less rigid – osmolysis.

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17
Q

Nebulised colistimethate sodium

A

Chronic colonisation gram neg pseudomonas aeruginosa as prophylaxis CF - rare eradicate chronic p.a * give regular use nebulized AB chronic p.a reduce r deterioration.

Use inhaled drugs target conducting upper airway tobramycin, colistin + aztreonam.

Broad spec polymyxins used against gram neg (except proteus) Polymyxins = polycationic + hydrophobic/ lipophilic molecules. Interferes cell membrane synthesis via LPS synthesis pathway
Ca2+ and Mg2+ displacement from LPS. Negatively charged LPS is unstable resulting in membrane leakage= bactericidal effect.
+ polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes.

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18
Q

Nebulized aztreonam

A

Gram neg aerobic – pseudomonas aeruginosa - targets conducting upper airway used prophylaxis

Monocyclic Beta lactam – high affinity PBP 3. Binds + inactivates PBP on inner cell membrane of bacterial wall. Inactivated PBP interferes cross linkage of peptidoglycan chains necc bacterial cell wall strength + rigidity. Interrupts bacterial cell wall synthesis * weakening wall + lysis.

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19
Q

Oral ciprofloxacin

A

Ciprofloxacin good permeation respiratory lower airway but bad upper – prophylaxis pa

Broad-spec (gram +/- AB fluoroquinolone Inhibiting DNA gyrase, and a type II topoisomerase, topoisomerase IV, necessary to separate bacterial DNA * inhibiting cell division.

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20
Q

Tacrolimus

A

Triple therapy for immunosuppression after bilateral lung transplant -tacrolimus, mycophenolate, prednisolone

Macrolide lactam
Inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12- prevents tranlocation NF * inhibiting t lymphocyte signlas + transcription Il-2,3,4,5.

Down regulates expression FceRI on langerhans

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21
Q

Mycophenate mofetil

A

Triple therapy bilateral lung transplant

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22
Q

Prednisolone

A

Triple therapy bilateral lung transplant

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23
Q

Tobramycin IV

A

Lower respiratory airway target pa

Broad spec Aminoglycoside against gram neg bacteria. Binds irreversibly 30s ribosome inhibiting formation 70s unit * bacterial protein synthesis.

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24
Q

Oral valganciclovir

A

Anti viral used combination therapy after lung transplant

Converted Ganciclovir after admin - phosphorylated to triphosphate form which is metabolized and taken in intracellurlarly.

Phosphorylation dependent on viral kinase + mainly occurs virus infected cells.

Ganciclovir triphosphate incorporated DNA strand replacing Adenosine * phosphodiester bridges can longer to be built, destabilizing the strand inhibiting viral DNA synthesis.

Also inhibits Viral DNA polymerase.

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25
Q

Oral co- trimoxazole

A

Combination therapy after bi-lateral lung transplant.

Antibacterial. Blocks folic acid enzymes in synthesis pathway. Sulfamethoxazole component inhibits formation dihydrofolic acid from PABA, trimethoprim component inhibits dihydrofolate reductase

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26
Q

Oral itraconazole

A

Antifungal against aspergillus funigatus colonisation

Interacts 14- alpha demethylase (cytochrome p-450 enzyme) converts lanosterol to ergosterol. Ergosterol is essential component fungal cell membrane * inhibiting synthesis = increase cellular permeability/ leakage cellular contents.

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27
Q

IV methylpredisolone

A

USE IF REJECTION OCCURS

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28
Q

Combination therapy after lung transplant

A

Combination therapy as infection prophylaxis nystatin, valgancyclovir, co-trimoxazole, colomycin and amphotericin for 4 months. one year after transplant, lower doses of tacrolimus, mycophenolate and prednisolone; infection prophylaxis reduced to co-trimoxazole daily

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29
Q

Budesonide side effects and indications

A

Asthma preventer - give reg when controlled reduce dosage

Adrenal supression
candidiasis + dysphonia

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30
Q

Budesonide mechanism

A

Inhibitory activities against
mast Cells, Eosinophils, Neutrophils, Macrophages, Lymphocytes, Histamine, Eicosanoids + Leukotrienes.
Binds to GR receptor, Corticoreceptor-Ligand complex translocate itself into the cell nucleus + binds to (GRE) in the promoter region of the target genes

The DNA bound receptor Interacts with TF -> increase/ decrease in expression of specific target gene

Suppression of IL2, Leukotrienes, Arachidonic Acid, Prostaglandins + IgE synthesis

Induce expression of IL-10, Lipocortin, Annexin 1

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31
Q

Salmeterol

A

LABA - prophalaxis 2x daily

Fine tremor + headache

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32
Q

Salmeterol mofa

A 
Stimulates beta (2)-adrenergic receptors via mimicking adrenaline
* relaxation of bronchial smooth muscles.

Beta2-Gs-Adenylate Cyclase. Increases cAMP production by activating Adenylate Cyclase. Increased intracellular cyclic AMP increases the activity of cAMP-dependent PKA
Inhibits the phosphorylation of myosin-light chain kinase and lowers intracellular calcium concentrations -> smooth muscle relaxation and bronchodilation

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33
Q

Salbutamol

A

Reliever short acting 30-60mins
Fine tremor
Headache
Reflex tachycardia

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34
Q

Salbutamol MofA

A 
Stimulates beta(2)-adrenergic receptors via mimicking adrenaline
* relaxation of bronchial smooth muscles.

Beta2-Gs-Adenylate Cyclase. Increases cAMP production by activating Adenylate Cyclase. Increased intracellular cyclic AMP increases the activity of cAMP-dependent PKA
Inhibits the phosphorylation of myosin-light chain kinase and lowers intracellular calcium concentrations -> smooth muscle relaxation and bronchodilation

Inhibits the release of bronchoconstricting agents from mast cells
+ Inhibits microvascular leakage
+ Enhances mucociliary clearance
Stimulus-independent

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35
Q

Beclometasone

A

Corticosteroid used COPD

Adrenal suppression + LRTI

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36
Q

Ipratropium

A

Anticholinegic agent- muscarinic receptor antagonist

Constipation + dry mouth

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37
Q

Beclometasone mechanism of action

A

Binds Glucocorticoid R. Inhibitory activities
mast Cells, eosinophils, neutrophils, macro, histamine, Eicosanoids, Leukotrienes + cytokines involved in allergic and non-allergic-mediated inflammation.

Inhibits phosphorylation of myosin-light chain kinase.

Bind to to IL-13 * inhibits function * inhibits class switching to IgE – needed coating mast cells.

Up-regulate b2-adreno-ceptor expression.

38
Q

Ipratropium mechanism of action

A

Blocks Muscarinic cholinergic receptors (M3-Gq subtype) * decrease formation cyclic guanosine monophosphate (cGMP)
Decreased activation on Phospholipase C+ formation of IP3 and DAG. Decreased PKC and IP3 and cGMP

Decrease intracellular calcium-> decreased contractility of smooth muscle.
Relaxation of bronchial smooth muscle + Inhibition of bronchial mucus secretion

Specific to parasympathetic bronchoconstriction

39
Q

Theophylline

A

Methylxanthine bronchodilator

Narrow theraputic window + vomiting

40
Q

Theophylline mofa

A

Relaxation of bronchial smooth muscle
Inhibition of cyclic nucleotide phosphodiesterase (PDE)

Less breakdown of cAMP, more cAMP
increases the activity of cAMP-dependent PKA, lowers calcium levels
* Inhibits the phosphorylation of myosin light chain kinase and lowers intracellular calcium concentrations -> smooth muscle relaxation and bronchodilation
Reduces airway responsiveness to histamine

41
Q

Drugs give prophylactic CF

A

Inhaled antibacterial drugs Aminoglycosides (tobramycin)
Polymyxins (colistin)
Monobactams (aztreonam)

Good permeation of upper conduction airway.
Poor permeation lower respiratory airway

Parenteral/ systemic administration of antibacterial drugs
IV 3rd gen cephalosporins (ceftazidime)
IV aminoglycosides (tobramycin)
Oral fluoroquinolones (ciprofloxacin)

Poor permeation of upper conducting airways
Good permeation lower respiratory airway

42
Q

Colistin indications and side effects

A

Severe Gram-negative, drug-resistant infections
Specific
Pseudomonas Acinetobacter

NOT Burkholderia, Proteus, Serratia, Neisseria (or anything Gram +ve)

Prophylaxis of colonisation in CF/COPD
Nephrotoxicity (tubular necrosis)
Neurotoxicity (can lead to respiratory failure) IV
Oral/inhaled (prophylaxis)

43
Q

Colistin mofA

A

Polymyxins interfere with cell membrane synthesis through the lipopolysaccharide synthesis pathway
Ca2+ and Mg2+ displacement from LPS. Negatively charged LPS is unstable resulting in membrane leakage

44
Q

tPA/ ALTEPLASE

A

Alteplase binds fibrin in clots via fibronectin finger like domain. Protease domain cleaves arg/val bond in plasminogen to form PLASMIN.

Plasmin degrades fibrin matrix of thrombus

45
Q

Warfarin

A

Inhibtis vit K reductase - reduction reduced form vit KH2.
Vit k is cofactor carboxylation glutamate residues on n terminal regions of vit k dependent proteins

  • limits gamma carboxylation and activation vit k dependent clotting factors
    II, VII IX X protein c/s
46
Q

Heparin

A

Binds endothelium reversibly - recruits + activates ATIII
UNfractionated heparin inactivates thrombin + factor X
also does II, IX,X, XII

LMW heparin only inactivates factor X

47
Q

Dalteparin

A

LMWH

Binds high affinity to plasma protein ATIII inhbiting formation factor Xa

48
Q

Dabigatran

A

INHIBITS THROMBIN

Rapid acting competitive + reversible direct inhibitor of thrombin (including free circulating thrombin, fibrin bound thrombin + thrombin induced platelet aggragation)
inhibitng thrmbin you inhibit platelet formation

49
Q

Rivaroxaban

A

Competively and irreversibly inhibits free + clot bound factor Xa which is needed to activate prothrombin to thrombin

50
Q

Clopidogrel

A

Anticoagulant - antagonistically binds P2y12 ADP receptor - needed aggregation platelets + cross linking protein fibrin.
Impairs ADP mediated activation GPIIb/IIA complex which is receptor for fibrininogen * impaired activation PREVENTS FIBRIN BINDING TO PLATELETS + INHIBITS PLATELET AGGREGATION

51
Q

What class is gentamycin

A

Aminoglyceride

52
Q

What class is ciprofloxin

A

Quinolone

53
Q

What is asprin used for

A

Irreversibly binds COX 1/2

Anti platelet reduce risk MI patient with angina

54
Q

MofA asprin

A

Acetlysalicyclic acid irreversibly inhibits COX 1/2 decrease formation prostaglandin + thromboxane from AA. Thromboxane A2 needed platelets aggregate - platelets cant synthesis new proteins + effect persists life platelet 7 days.

55
Q

Indications Atenolol

A

BETA BLOCKER - allows decrease O2 demand due reduction HR + contractility - relief ischemic chest pain

Early intervention MI (12hrs) esp if STEMI

56
Q

MofA atenolol

A

Binds B1 adrenergic receptors in heart + vascular SM.
inhibits sympathetic Stimulation * reduction reduction resting heart rate, CO, SBP + reflex orthostatic hypotension.

Higher does also block B2 bronchial + vascular SM

57
Q

What is clopidogrel

A

Anti platelet reduced death after MI
Clopidogrel + asprin indicated STEMI

Nausea + vomiting

58
Q

MofA clopidogrel

A

Impairs ADP mediated activation glycoprotein GPII/IIIa complex (receptor for fibrinogen). Impaired activation prevents fibrinogen binding platelets + inhibits platlet aggregation.

59
Q

What is simvastatin

A

Lower cholesterol via inhibitng HMG- CoA reductase

potentially reduce risk second stroke

60
Q

Mechansim simvastatin

A

SELECTIVELY INHIBITS HMG-CoA reductase in liver * inhibits formation mevalonic acid (rate limiting step in synthesis cholesterol) * reduction cholesterol levels + increase expression hepatic LDL receptor

61
Q

Indications ramipril

A

Lower blood pressure ACE inhibitor

62
Q

Mechansim ramipril

A

ACE inhibitor
Blocks conversion angiotensin I to angiotensin II
Angiotensin II vasocontrictor + stim release aldosterone * if inhibit production vasodilation + inhibition salt + water retention

63
Q

What is Warfarin used for

A

Prophylaxis against dev new blood clots

64
Q

MofA Warfarin

A

Inhibits vit K reductase enzyme * inhibit synthesis vit k dependent coagulation factors (II, VII, IX X) decrease coagulation factors get lowering prothrombin levels - reduced thrombin + fibrin - > reduced clotting

65
Q

Morphine

A

Activates μ opioid receptors (Gi protein coupled) in the brain (thalamus, limbic system + PAG) and spinal cord dorsal horn . Also acts on delta receptor in limbic system, cortex + dorsal horn. And kappa receptors in cortex and dorsal horn. When binding opioid receptor inhibition adenylate cyclase activity, decrease cAMP open K+ channels (potassium diffuse out into synaptic cleft making it less likely A.P to be fired – post synaptic hyperpolarization) Inhibit the opening of Ca2+ channels in nerve endings – reduce release neurotransmitter.
Act directly on dorsal horn inhibiting the transmission of pain signals and by decreasing excitation peripheral nociceptive afferent neurons.

Stimulate the descending inhibitory pathways (supra-spinal analgesia) via PAG and NRPG which release enkephalin -synapses with Raphe magnus. Neurons arising from RM terminate DH releasing serotonin causing local neurons secrete endorphins * inhibition pain. inhibits sensory nerve transmission to spinal ascending pathways (spinal analgesia)

66
Q

Paracetamol

A

Paracetamol – inhibits Cox I in hypothalamus = antipyretic action + weak inhibition peripheral cox isoforms ( * not used peripheral inflammation). Activation serotoninergic pathways. Little suppression of inflammation but good control of inflam pain.
Paracetamol metabolite inhibits reuptake of anandamide and increases activity cannabinoid receptors and TRPV1.

67
Q

Gardasil

A

®: VLP of HPV6,11,16,18

68
Q

Cervarix

A

VLP 16 18

69
Q

What is amlodipine

A

Calcium channel blocker -> decrease her blood pressure via vasodilation + decrease pacemaker potential.

70
Q

What is oral phenoxy benzamine

A

Irreversibly blocks Alpha receptors * Inhibits Alpha 1-Gq mechanism - lower BP

71
Q

What is atenolol

A

Beta blocker

Inhibits sympathetic stimulation to lower HR and BP

Short acting

72
Q

MOFA Amlodipine

A

Long Acting
Inhibits Calcium ion influx via L-type calcium channels -> stabilisation of channels in inactive conformation
Decreased (d) calcium binding to Calmodulin (calcium binding protein) -> d activation of MLCK
-> d phosphorylation of MLC
-> d CICR -> d arterial smooth muscle contractility * vasoconstriction -> VASODILATION -> decrease TPR -> decrease in BP

Inhibition of carbonic anhydrase = increases pH , regulate calcium influx + inhibits this in the SAN/AVN heart-decreases pacemaker potential
* d HR + inhibits this in myocytes, decreased force contraction -> decreased SV.

73
Q

MofA oral phenoxy benzamine

A

Irreversibly blocks Alpha receptors * Inhibits Alpha 1-Gq mechanism
-> d activation on Phospholipase C -> d formation of IP3 and DAG -> d PKC and IP3 and cGMP -> d intracellular calcium -> d Contraction -> muscle relaxation + widening of the blood vessels * lowering of blood pressure.

Competitive irreversible antagonist of adrenaline – binds adrenaline receptors * less available adrenaline to act upon.

74
Q

Mof A atenolol

A

Competes with sympathomimetic neurotransmitters (catecholamines) via binding beta (1)-adrenergic receptors in heart/ vascular smooth muscle * Inhibits sympathetic stimulation -> reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Higher doses atenolol competitively block beta (2)-adrenergic responses in the bronchial and vascular smooth muscles.

75
Q

PODOPHYLLOTOXIN

A

Soft non keratinised warts
Blocks cell division via inhibition micro-tubule assembly in mitotic apparatus

Inhibits topisomerase II during S phase - bind and stabilize temporary break and disrupt reparation break - stopping DNA unwinding and replicating

76
Q

Topical imiquid

A

larger keratinised warts

Allows innate + acquired IR recognize abnormal cells - inflam cell infiltration + apoptosis of diseased tissue.

induces expression Il-6, Il-8 + TNF alpha

Stim apoptosis in BCC cells

77
Q

TCA

A

Trichloroacetic acid - chemically burns wart

78
Q

Effects of adrenaline

A

Alpha 1 vasocontriction skin, kidney + brain
Beta 1 increase CO increase contractility HR + conduction
Beta 2 vasodilates + bronchodilates

Increase BP via stim alpha 1 > beta 2

79
Q

What is the reflex bradycardia in response to adrenaline

A

NA stim Beta I increasing myocardium contractility but reflex mechanism do decrease HR. NA causes ABP + stroke vol to increase - strim baroreceptors in aorta - vagus centre. Reflex vagus bradycardia negates influence B1 R * CO not significantly changed

80
Q

Heceptin/ Trastuzumab

A

IgG1 monoclonal AB selectively binds high affinity HER2 proto-oncagene -> AB mediated killing HER2 +ve cells - induce arrest G1 phase cell cycle * reduced proliferation

81
Q

Dexamethasone

A

Glucocortiocoid receptor agonist. Binding GR loses inhibitory proteins translocation cell nucleus binds GRE on promoter region target genes - interacts TF up regulate/ down regulate expression target gene.

Supression Il-2 leukotrienes AA + prostaglandins.
Phosphoylates annexin I
Inhibits leukocyte infiltration

82
Q

Beta interferon

A

Endogenous IFN B contributes mediation anti inflam + regenerative effects. Binds type 1 IFN R - activate JAK 1 - phosphorylate receptors - bind stat 1/2. Dimerize + activate immunoregulatory + anti viral proteins.

increase production neuronal growth factor + inhibit leukocyte migration across BB

83
Q

Amoxicillin

A

Beta lactam
PBP 1a - inactivation transpeptidase * inhibits peptidoglycan polymer cross linking.

First line gram +ve
Pseudomonas + enterobacteriacae resistant

84
Q

Ceftazidime

A 
Broad spec beta lactam 
Inhibits PBP3 (Beta lactam ring mimics d-ala- d ala dimer between NAM) - inactivation transpeptidase * inhibits peptidoglycan polymer cross linking. Cell lysis mediated autolytic enzymes.

Staphylococci resistant

Good pseudomonas + E coli

85
Q

Gentamicin

A

Aminoglyceride broad spec gram neg

Irreversibly binds 16S ribsosomal RNA within 30s sub unit. Interference INITIATION COMPLEX. Misreading mRNA * incorrect aa inserted polypeptide - non functional peptides * bacteria cant synthesize proteins for growth.

86
Q

Ciprofloxacin

A

Quinolone - broad spec
Inhibits Topoisomerase II/DNA gyrase and Topoisomerase IV - Inhibition uncoiling & unwinding of DNA from histones -> required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination

Inhibits DNA replication
Good for Pseudonomas aeruginosa

87
Q

Codeine

A

Converted into morphine
Selective Mu R (GPCR I) weaker than morphine. Bound inhibits AC * reduction cAMP. Acts on reticular formation, limbic system + PAG. Stim release endorphins (enkaphaline/ 5-HT). STIMULATES DESCENDING INHIBITORY PATHWAYS.

Inhibit sensory nerve transmission via substance P (c fibers)
Moderates integration processes in limbic system

REDUCES NEURONAL EXCITABILITY AND NEUROTRANSMITTER RELEASE.

88
Q

Vancomycin

A

Glycopeptide

binds d ala- d ala blocking action transpeptidases

89
Q

Stages clot formation

A 
propagation
organisation
Re- canilzation
Embolism
Resolution
90
Q

Tpa

A

binds thrombus - conformational change allows conversion plasminogen to plasmin

Year 2 (12 decks)

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