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STUDY FOR BARRIERS > Pharmacology 😎 > Flashcards

Pharmacology 😎 Flashcards

1
Q

Chemotherapy following surgery is

A

Adjuvant

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2
Q

Chemo prior to surgery is

A

Neoadjuvant

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3
Q

Cytotoxic chemo - 6 key features?

A

Cell kill

Kill mechanism - cell cycle specific or not

Administer cyclically

Give as combinations

Resistance

Dose intensity / toxicity

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4
Q

In a medium size tumour what percentage of cells are actively dividing?

A

5%

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5
Q

Why is chemo given in cycles?

A

Drug target and injury rapidly dividing cells but are not cancer specific (normal cells also affected)

Rest periods allow normal cells to recover and body to regain strength

Cancer don’t repair so easily

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6
Q

Why is chemo given in combination?

A

To enhance cell kill and decrease chance of resistance without additive toxicity

Use drugs active to tumour type and with different mechanisms and with non-overlapping dost-limiting toxicities and used at optimum stages

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7
Q

Resistance to chemotherapy drugs can occur due to

A

In-built protecting to toxins (genetic resistance)

Spontaneously

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8
Q

Mechanisms of cytotoxic resistance :

A 
Reduced accumulation in cells 
Decreased uptake in cell and increase intracellular breakdown
Bypass biochemical pathways 
Utilise alternative gene amplification 
Overproduction of blocked enzyme 
Rapid repair to damaged DNA
Genetic mutations
Genetic resistance
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9
Q

Main possible side effects of chemotherapy

A 
Anaemia 
Infection
Nausea and vomiting 
Neutropenia
Skin reactions 
Thrombocytopenia
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10
Q

Alkylating agents

A

Cisplatin
Interfere with DNA base pairing, leading to strand breaks and arresting replication
Attach alkyl group to guanine base
Effects manifest during S phase –> block at g2 and apoptotic cell death

Toxicity:
Myelosuppression
N&V
Haemorrhagic cysts (due to bladder fibrosis and pulmonary fibrosis )

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11
Q

Antimetabolites

A 
Gemcitabine
Methotrexate (Lower dose as dMARD) 
Either direct inhibition of enzymes needed for dna replication or repair OR incorporation of an Antimetabolite directly into dna (disrupts structure and function)
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12
Q

5-fluorouracil

A

Antimetabolite
Pyramidine antagonist

Given with folic acid

Binds to thymidylate synthetase

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13
Q

Anthracyclines

A

-rubicin
Epirubicin
Cell cycle non specific
Inhibit dna replication and therefore cell division

Inhibit Dna and rna synthesis by intercalating between base pairs

Inhibit topoisomerase II preventing relaxing of recoiled dna blocking transcription and replication

Produced reactive free radicals

Toxicity:
Cumulative cardiotoxicity
The usual

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14
Q

Antimicrotubule agents

Taxanes

A

Bind to tubulin
Interfere with microtubules
Blocks cell growth by stopping mitosis

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15
Q

P glycoprotein is

A

An inbuilt mechanism for multi-drug resistance

Responsible for decreased drug accumulation in multi drug resistant cells and often mediates the development of resistance to anticancer drugs

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16
Q

Targeted cancer therapy includes

A

Monoclonal antibodies
Small molecule drugs
Angiogenesis inhibitors
Drugs targeting apoptosis

Combines with chemo

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17
Q

Monoclonal antibodies

A

Not cytotoxic
Target on cell surface of target extra cellular components

The more mouse the more chance of hypersensitivity reaction
Premedication- antihistamine and corticosteroids

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18
Q

EGFR antagonists

A

Epidermal growth factor
Cutaneous reactions

Cancer

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19
Q

Main antiemetic options

A

Serotonin antagonists
Dopamine antagonists
NK1 blocker
Anticholinergics

Corticosteroids

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20
Q

Dopamine antagonists

A

Metaclopramide
D2 antag with 5HT3 and 5HT4 agonist activity

Central - blocks d2 in CTZ
Peripheral - blocks 5ht3 (blocks vagus nerve going to CTZ) and agnostic 5ht4 (increased gastric emptying)

AEs: extrapyrimidal symptoms, galactorrhea

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21
Q

5HT3 antagonist

A

Ondansetron
Selective
Blocks in cns and periphery
Potent

AEs: QT prolongation

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22
Q

Aprepitant

A

Oral NK-1 antagonist
Selective
Can penetrate brain - used in brain tumours

Usually combined with ondansetron/dexamethasone a steroid to help brain penetration

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23
Q

Treatment for mucositis

A 
Oral hygiene: 
Salt mouthwash
Chlorhexidine (antiseptic) 
NSAIDs (for pain and other areas)
Palifermin - recombinant human keratinocyte growth factor, binds to KGF receptor

Common in patients on 5-flurouraciln

Lignocaine - local anaesthetic to reduce pain - blocks na channels

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24
Q

Management of diarrhoea

A

Opioids - mu receptor agonists

  1. Codeine (cns and periphery )
  2. Diphenoxylate or loperamide (Imodium) - peripheral only

Somatostatin

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25
Octreotide
Somatostatin Octreotide acetate Decreases GIT transit time and endogenous fluid secretion in jejunum Stimulates intestinal absorption of water and electrolytes Treatment of diarrhoea and radiation-induced colitis
26
G-CSF
Filgrastem/peg-filgrastem Decreased risk of febrile neutropenia in myelosuppressive chemo Autometabolised by neutrophils AEs: bone pain Given only in FN risk 20% or more
27
Darbopoietin alpha
Acts on RBCs Indication - chronic myelosuppression post chemo
28
Treatment for recurrent oral thrush
Nystatin oral drops (antifungal)
29
-ciclovir
Aciclovir Valaciclovir Famciclovir DNA polymerase inhibitors Antivirals
30
Tumour lysis syndrome can lead to
Hyperuricemia
31
Treatment for hyperuricemia
Xanthine oxidase inhibitor - allopurinol Urate oxidase - rasburicase (Uric acid --> allantoin
32
Anti platelet agents act on
Primary haemostasis
33
Anticoagulant acts on
Secondary haemostasis
34
Antimalarial used to prevent relapse
Primaquine
35
Main antimalarials
Chloroquine | Quinine
36
Aspirin
Antiplatelet Inhibits prostaglandin Inhibits prostacyclin and thromboxane a2 but more txa Inhibits platelet activation and
37
Dipyridamole
Anti platelet Inhibits PDE in platelets and in vessels Vasodilation and
38
Mode of action to COC:
Oestrogen inhibits fsh via neg feedback --> suppresses development of ovarian follicle Progesten inhibit release of LH --> prevent ovulation and thicken cervical mucus Both together --> alter endometrium to discourage implantation
39
Progesten only pill acts on
Mainly the cervical mucus | Maybe some effect on endometrium and motility and secretions of Fallopian tube
40
Postcoital (emergency) contraception treatment with
Levonorgestrel Within 72 hr Repeated 12hr later Or IUD - affective for up to 5 days
41
What is the dose of oestrogen needed to be effective in contraceptive pills?
At least 20 micrograms No more than 50 Standard dose is 30-35
42
Contraceptive pills | Monophasic formulation?
Fixed dose of oestrogen and progestogen for 21 days
43
Contraceptive pill | Triphasic formulation?
3 phases with progesterone "step up" in phase 3 More closely mimics hormone changes during menstrual cycle Reduce breakthrough bleeding
44
Contraceptive pills | Quadriphasic formulation?
4 phases of oestrogen step down , progestogen step up regimen
45
P2Y12 receptor blockers
Clopidogrel - irreversible inactivates receptor Ticagrelor - reversible ADP receptor p2y12 inhibitor Rapid onset action (2-4hrz)
46
Glycoprotein IIb/IIIa blockers
Blocks platelet aggregation Abciximab Very expensive
47
Warfarin
Vitamin k antagonist Low therapeutic index but reversible with vitamin k Target INR = 2-3 Need monitoring Anticoagulant
48
Heparins
Anticoagulant Indirect thrombin inhibitors Reversibly inhibit Basically inactivates all factors except 13 lol
49
Unfractionated vs LMW heparin
``` LMW: works more on factor Xa Doesn't inhibit platelet function Renal elimination Monitoring generally not needed but Xa assay can be done which is difficult ``` ``` Unfractionated: Inhibits platelet function Equally anti Xa and IIa Renal and hepatic elimination Monitored with APTT frequently Rapid onset and clearance ```
50
Direct thrombin inhibitor
Dabigatran Oral No antidote Renal elimination
51
Factor Xa inhibitors
``` Rivaroxaban Apixaban Oral Directly factor Xa inhibitors Can get away with lower renal function than dabigatran and won't accumulate ```
52
NOACs
Novel oral anticoagulants Dabigatran Rivaroxaban
53
Fibrinolytic agents
T-PA eg alteplase Tenecteplase Dissolves existing thrombus Activates plasminogen Used when clot already formed in patient Within 3 hrs of stroke AEs: works too well
54
Beta lactams mechanism of action
Penicillins and cephalosporins Amoxicillin (+clavulanic acid) Bactericidal Interfere will cell wall peptidoglycan synthesis (inhibits the enzyme that cross links the peptide chains
55
Penicillins
``` Narrow spectrum: Active against gram +ve Haemophilus influenzae Otitis media Inactivated by beta lactamses produced by staphylococci Benzylpenicillin ``` Anti staphylococcal: Methicillin Flucloxacillin Methicillin resistant staph aureus - resistant to all beta-lactams ``` Broad spectrum: Greater activity against gram -Ve E. coli, h influenzae Destroyed by beta lactamases producing strains Amoxycillin, ampicillin ``` Anti-pseudomonal: Pseudomonas aeruginosa Piperacillin, ticarcillin
56
Beta lactamase inhibitors
Clavulanic acid Tazobactam Inhibit enzymes prod by staph aureus, bacteroides fragillis, and E. coli
57
Cephalosporins
First generation: Cephalexin Active against penicillinase prod staph, and gram -ve s like E. coli and klebsiella (enteric rods) Not active against some gram negative anaerobes like bacteroides fragillis and some enterobacter or pseudomonas spp 2nd generation: Cephamandole, cefoxitin More stable to gram neg beta lactamase a 3rd gen: Ceftazidime, cefpirome Cover majority of gram negative rods Able to enter CSF
58
Tetracyclines
Reversibly bind to 30s subunit of microbial ribosomes and blocks attachment of transfer-RNA to the A site on ribosome, prevents introduction of new amino acids to peptide chain Doxycycline Tetracycline Bacteriostatic Broad spectrum Most commonly used in skin infections
59
Amino glycosides
Gentamicin Conc-related bacteriocidal effect Inhibit protein synthesis by promoting misreading of DNA Gram negative spectrum including pseudomonas aureginosa Monitor for nephrotoxicity and ototoxicity
60
Sulfonamides
Analogues of PABA Compete for enzyme dihydropteroate synthetase (needed for folic acid synthesis in bacteria) Bacteriostatic Sulphamethoxazole (Comb with trimethoprim- dihydrofolate reductase inhibitor)
61
Trimethoprim
Folate antagonist Bacteriostatic Dihydrofolate reductase inhibitor Usually: PABA --> folate --> tetrahydrofolate and then DNA
62
Quinolones
Ciprofloxacin Norfloxacin Analogues of nalidixic acid Bactericidal Inhibits nucleic acid synthesis Inhibitor of DNA gyrase (coils DNA) and topoisomerase ``` Broad spec Basically - Gram negatives Pseudomonas aureginosa H influenzae Poor activity against streptococci ``` AEs. Achilles tendinitis
63
Macrolides
Erythromycin Azithromycin Clarithromycin Broad spec Gram pos and neg cocci and anaerobes but not gram negative rods Maybe cidal or static depending on conc Inhibits protein synthesis by binding to 50s ribosome Nausea (Erythromycin Resembles motilin )
64
Nitroimidazoles
Metronidazole Cidal Gram negative anaerobes such as bacteroides fragillis Protozoa And some gram pos Significant interaction with alcohol
65
Glycopeptides
Vancomycin Cidal Inhibit cell wall synthesis Narrow spec Gram pos aerobic and anaerobic organisms Used in MRSA
66
Centrally acting sympatholytics (CV drugs)
Clonidine (presynaptic a2 agonist) Alpha- methyldopa (Inhibits dopa decarboxylase to decrease dopamine prod and stimulates presynaptic a2 adrenoceptors
67
Beta blockers
Propranolol - nonselective beta 1 and 2 Metoprolol - b1 antagonist (will give less bronchoconstriction)
68
Alpha1 blockers
Prazosin (alpha1 adrenoceptor antagonist) --> vasoconstriction to NA Arterial and venous dilation (decreased TPR and venous return (decreased contractility and CO and therefore, BP)
69
Non selective alpha blocker causes
Reflex tachy As blocking a2 stops the negative feedback loop and increases NA which acts on b1 on heart muscle as a1 (vascular smooth muscle) is also blocked
70
Loop diuretics
Frusemide Acts on ascending loop Inhibit na/k/Cl carrier Prevent transport of nacl from tubule Potent, 4-6hrs
71
Thiazide diuretics
Hydrochlorothiazide Act on DCT Inhibit na/Cl transport system Short term - decrease plasma volume Long term- direct vascular effects by action on K channels Most commonly used for HT and mild heart failure AE: can worsen diabetes (hyperglycaemia)
72
Potassium sparing diuretics
1. Amiloride Block na channels on last part of DCT and collecting tubules Therefore, decreased K+ excretion 2. Spironolactone Same thing by antagonising aldosterone Can affect other steroid receptors --> menstrual disturbances Used in comb with K losing agents Both cause limited diuresis
73
ACE inhibitors
Perindopril Inhibit A2 mediated vasoconstriction and release of aldosterone AEs: dry cough
74
AT receptor blockers
Irbesartan Block AT1 receptor subtype AEs: less cough and hypotension
75
Drugs to produce peripheral vasodilation
Calcium antagonists: Depress contractility directly Nitric oxide donators: Induce dilation
76
Calcium channel antagonists
Dihydropyridines: Amilodipine, nifedipine More effective on vascular muscle -->peripheral vasodilation Indications : hypertension AEs: flushing, headache, ankle swelling, palpitations (reflex tachy) (increased SNS activity) Non-dihydropyridines: Verapamil, diltiazem More effective on heart (dilate coronary arteries, inhibit AV node conduction, reduce cardiac contractility) Indications: angina Contraindications: HF as can cause heart block and negative inotropy
77
The 5 main classes of drugs used to treat hypertension
``` Calcium channel blocker Ace inhibitors ARBs Beta blockers Diuretics ``` Usually start with beta blocker and thiazide diuretic Complementary comb therapy eg ace inhibitor and diuretic
78
Atropine is used in
Sinus bradycardia | To dilate pupils
79
Adrenalin is administered in which cardiac event
Cardiac arrest
80
Isoprenaline is used in which cardiac problem
Heart block
81
Digoxin is used for
Rapid atrial fibrillation
82
What do you administer for ventricular tachycardia due to hyperkalaemia
Calcium chloride
83
What is used for VF and digoxin toxicity?
MgCl2/MgSO4
84
Class 1 antyarrythmics
Na channel blockers Reduce rate of depol during phase 0 Inhibit AP in excitable cells --> decreased conductivity and contractility Dependent channel block (use dependence) - bind most when channels in open or refractory state
85
1A antiarrythmic
Quinidine Procainamide Slow phase 0 Lenghten AP Prolong refractory period Prolong QT Use: ventricular arrhythmias (eg VT) AEs incl mild anticholinergic effects
86
1B antiarrythmic
Lignocaine Use dependence Shortened depol Decrease AP duration Use: severe ventricular arrhythmias Precautions - HF, bradycardia (weak inotropes)
87
1C antiarrythmic
Flecainide High affinity for open channel and very slow dissociation No effect on AP duration Reduce automacity, reduce AV conduction and contractility AEs : QT prolongation Negative inotrope
88
Class 2 antiarrythmic
Beta blockers Metoprolol, atenolol Block catecholamines activations of beta receptors AND depress phase 4 depol of pacemaker cells Inhibit SNS activation and cause indirect Ca2+ inhibition (on phase 2) Decrease HR Prolong PR interval (atrial depol) Increase RO and prolong AP by decrease conduction through AV node Use: prevent tachys Eg SVT and paroxysmal AF Provoked by SNS eg AMI and exercise
89
Class 3 antiarrythmic
Sotalol Amiodarone Block K+ channel Substantially extend AP and RP without affecting phase 0 Prolong RP and QT& PR intervals Use: supraventricular and ventricular tachys
90
Sotalol
Non selective beta blocker and k channel blocker Prolongs AP and QT and RP Use: SVT, AF, VA Contraindications: asthma, sinus bradycardia, prolongs QT, sever HF Accumulates in renal impairment
91
Amiodarone
Class 1, 2, 3 and 4 effect Prolong QT! Long half life Many side effects! Incl photosensitivity, pulmonary fibrosis!, corneal deposits, N&V, blue grey discolouration of skin
92
Class 4 antiarrythmic
Calcium channel blockers Verepamil and diltiazem Slow AV conduction and increase RP Suppress premature ectopic beats L type channels Negative inotrope and chronotrope Also decrease BP ``` Contraindications - Bradycardia HF Oedema Constipation (verapamil) Headache and dizziness and fatigue ``` Use: predominantly for SVTs and angina but now prefer IV adenosine for acute episodes
93
All antiarrythmics should be avoided in sever heart failure except
Amiodarone | Digoxin
94
Drugs for atrial fibrillation
DC shock or drugs: Use drugs that increase block at AV node Acute - Sotalol or amiodarone Maintainers: beta blocker or amiodarone Normal LVF: Beta blockers or calcium channel blockers LV dysfunction: Digoxin (often ineffective) or amiodarone
95
Digoxin
Cardiac glycoside Narrow therapeutic range Renal clearance Long half life Useful in LV dysfunction, HF Cardiac slowing Increase RP - reduces ventricular rate Slowing rate of conduction through AV
96
Drug therapy for SVT
Adenosine (slows AV conduction and also produces peripheral and coronary vasodilation) (*can precipitate bronchospasm) If fails --> verapamil Prevention: Choose drug that blocks at AV node Verapamil, digoxin, beta blocker Sotalol, amiodarone
97
NO donors
``` Relax smooth muscles via cGMP mediated activation of PKG Dilate peripheral arteries and veins Decrease venous return Decrease preload and after load Reduce demand on heart ``` Short acting - glyceryl trinitrate Activated by mitochondrial aldehyde dehydrogenase-2 at low conc Long acting - isosorbine dinitrate or mononitrate High concentrations --> high potency Low potency activated by p450 enzymes Reflex tachycardia evoked (Stop with beta blocker?) Tolerance and "pseudotolerance"
98
Treatment for reducing CVS risk
1. NO donor 2. Aspirin/anti platelet 3. Statins 3.
99
Adverse affects of statins
Myopathy: Myalgia + increased CK Rhabdomyolysis: Severe muscle pain assoc with serum CK > 40 times upper limit Rare but potentially fatal Skin rashes ``` GIT: Cramps Constipation Diarrhoea Heartburn ``` drug interactions Warfarin Higher incidence of myopathy with CYP inhibitors
100
Fibrates
``` Activate PPAR (peroxisome proliferator- activated receptors) (modulate carb and fat metabolism) Increase activity of lipoprotein lipase and decrease synthesis of apoC-III together enhance clearance of circulating TG-rich lipoproteins ``` Gemfibrozil or fenofibrate Decrease TG by 40% Increase HDL by 10-20% AEs: Myopathy Increase gallstone risk and increased cholesterol in bile Blood dyscrasias Photosensitivity Drug interaction (increased bleeding risk with warfarin
101
Adenosine diphosphate is
Released from platelet dense granules and injured cells Bing to P2Y1 (platelet aggregation) and P2Y12 (platelet activation) Induces activation of GP2b/3a receptor and platelet aggregation Inhibited by clopidogrel
102
Acute uncomplicated UTI/cystitis
``` Trimethoprim 3d Cephalexin Amoxicillin/ clavulanic acid Nitrofurantoin 5d Men - 7d ``` Pyelo - increase duration 10-14 d or frequency If ESBL producing: Meropenem
103
Prophylaxis of recurrent UTI
Ph modifiers Acidifiers- ascorbic acid (vit c) or Cranberry juice (contains proanthocyanidines (inhibit adhesion of fimbriae) and fructose) Alkalinisers - citric acid or tartaric acid or sodium bicarbonate (relieves discomfort on urination but not prophylaxis benefit) Continuous Intermittent self treatment
104
Urinary antiseptics
Require acidic urine for activity H examine hippurate Hexamine mandelate
105
Which drugs would cover e.coli or staph sap uti ?
Trimethoprim | Cephalexin

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