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F****** Pharmocology > Student Formulary Drugs > Flashcards

Student Formulary Drugs Flashcards

1
Q

When would you prescribe Activated Charcoal

A

Paracetamol overdose or aspirin (salicylate) overdose- if <1hr since ingestion

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2
Q

What would you treat a paracetamol overdose with?

A
  1. Activated charcoal (if less than 1hr since taking overdose)
  2. N-acetylcysteine if 4hr paracetamol level is above treatment line or if below normal treatment line but considered high risk

(High risk = on p450 inducer medications (phenytoin, carbamazepine, rifampicin, St Johns wart), alcoholic, HIV+ or malnourished (glutathione depletion))

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3
Q

What would you treat an aspirin overdose with?

A
  1. Activated charcoal if less than 1hr since overdose
  2. Alkalinise urine using sodium bicarbonate +/- potassium chloride - often no longer used
  3. Haemodialysis - 1st line if pulmonary oedema /severe poisoning
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4
Q

On an ABG what would an aspirin overdose look like?

A 
Metabolic acidosis with respiratory alkalosis for compensation
pH <7.35
PaO2 high
PaCO2 low 
Bicarb low
BE low
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5
Q 
Patient arrives in A&E breathing extremely rapidly. You do an ABG. These are the results:
pH 7.1
PaO2 12
PaCO2 2.65
Bicarb 4.7
BE -29.2
What do you suspect?
A

Metabolic acidosis with respiratory alkalosis for compensation. Potentially a salicylate overdose

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6
Q

Docusate sodium - MOA?

When is it contraindicated

A

Stimulate laxative - increases intestinal motility

CI: bowel obstruction

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7
Q

What are examples of stimulant laxatives?

When are they CI?

A 
Docusate sodium
Glycerin (PR)
Senna
Picosulfate
CI: bowel obstruction
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8
Q

What is a glycerin enema used for? MOA? CI?

A

constipation
stimulant laxative
CI: bowel obstruction

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9
Q

Senna

A

stimulant laxative

CI: bowel obstruction

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10
Q

Picosulfate

A

stimulant laxative

CI: bowel obstruction

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11
Q

Bran. MOA? SE? CI?

A

Bulking agent - increase faecal mass and therefore increase peristalsis
SE: bloating
CI: bowel obstruction

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12
Q

Ispaghula. MOA?SE? CI?

A

Bulking agent - increase faecal mass and therefore increase peristalsis
SE: bloating
CI: bowel obstruction

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13
Q

Examples of bulking agents used in constipation?

A

Bran

Ispaghula

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14
Q

What are examples of osmotic laxatives? When are they contraindicated?

A 
Lactulose 
Macrogel
Phosphates
Mg Salts
CI: bowel obstruction
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15
Q

What is lactulose? What is it used for?

A 
Osmotic laxative - increases water content of stools. 
Used in:
- constipation
- hepatic encephalopathy
(CI: bowel obstruction)
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16
Q

What is an example of a stool softener?

A

liquid paraffin

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17
Q

What is liquid paraffin?

What are its side effects

A

stool softener. used in constipation.
SE: decreased absorption of ADEK vitamins (Fat soluble)
Granulomatous reactions

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18
Q

What is a phosphate enema used for? How does it work?

A

Constipation. It is an osmotic laxative - increasing the water content of the stool

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19
Q

What is gaviscon and when is it used?

A

Gaviscon = alginate

Used in GORD
Decreases reflux by increasing the viscosity of the stomach contents. It forms a raft on top of stomach contents

Can be bought OTC

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20
Q

What are examples of antacids and when are they used?

A

Mg Trisilicate
Al hydroxide
They are used in dyspepsia, GORD and PUD. They neutralise gastric acid.
Take when symptoms occur / are expected - PRN
They can interfere with drug absorption

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21
Q

Constipation is a side effect of which antacid

A

Al hydroxide

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22
Q

Diarrhoea is a side effect of which antacid

A

Mg trisilicate

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23
Q

Movicol - what is it ? How does it work? When should you not give it?

A

Osmotic laxative + potassium chloride, sodium chloride and sodium bicarbonate. Comes in a sachet that you mix with water and drink.
Works by increasing the water content in the stool.
Should not be given if you suspect bowel obstruction - so if patient is distended, constipated, severe pain, vomiting etc..

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24
Q

Omeprazole, lanzoprazole, pantoprazole. How do they work?

A 
Proton pump inhibitors 
Activated in acidic pH
Irreversibly inhibit H+/K+ ATPase 
More effective than H2 antagonists such as ranitidine
May mask symptoms of gastric cancer
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25
Q

Side effects of PPIs

A

Headache

GI disturbance

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26
Q

What do PPIs interact with

A

p450 inhibitors e.g. many antibiotics, isoniazid, cimetidine, sodium valproate, chloramphenicol

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27
Q

Ranitidine, cimetidine. MOA?

A

H2 receptor antagonist

Decrease gastric parietal cell H+ secretion

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28
Q

Cimetidine. SE? Interactions?

A

GI disturbance
Interact with p450 inhibitors e.g. isoniazid, chloramphenicol, sodium valproate
May mask symptoms of gastric cancer

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29
Q

What is often given with NSAIDs to prevent PUD?

A

Misoprostol - prostaglandin analogue
Acts on parietal cells to decrease H+ secretion.
Common SE : diarrhoea

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30
Q

ACEI - ramipril, lisinopril, enalapril. What are they used for?

A 
HF
HTN
Post-MI
Angina
Diabetic nephropathy
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31
Q

What are the SEs of ACEI

A 
hypotension
renal failure
increased potassium
Dry cough: 10-20% - due to increased bradykinin
Angioedema (~0.1%)
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32
Q

When are ACEI contraindicated?

A

Bilateral renal failure
Angioedema/hypersensitivity to ACEI
Salt substitutes (containing K+)
Pregnancy

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33
Q

What does ramipril interact with?

A

Increased risk of RF in patients on NSAIDs
Diuretics, TCAs and antipsychotics - risk of hypotension
Caution with drugs that increase K+ e.g. spironolactone

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34
Q

What needs to be monitored on ACEI?

A

U&Es - an increase in creatinine >30% -stop
titrate dose
avoid in young women likely to become pregnant - consider beta-blocker.
decrease dose in renal failure

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35
Q

What is the MOA of losartan

A

Angiotensin receptor blocker - do not inhibit bradykinin breakdown so no cough

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36
Q

What are the SE of ARBs

A 
Same as ACEI:
Hypotension
Increased K+
Renal failure
Angioedema (~0.1%)
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37
Q

Contraindications of ARBs

A

Caution in RF

Do not use in pregnancy

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38
Q

Interactions of losartan?

A

Hypotension- risk with diuretics, TCAs and antipsychotics
Increased risk of renal failure with NSAIDs
Caution when using in patients on drugs that increase K+ e.g. spironolactone

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39
Q

Patient has recently been started on a new drug and begins to find breathing more difficult and swelling of his tongue. What would you prescribe?

A

High flow oxygen through a non-rebreathe mask
Adrenaline 0.5ml of 1:1000
Chloramphenamine 10mg IV
Hydrocortisone 200mg IV
Nebulisers: salbutamol 5mg and ipratropium 0.5mg

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40
Q

Bendroflumethiazide - MOA?

A

Thiazide diuretics - acts in distal convoluting tubule.

Inhibits NaCl transporter and therefore increases excretion of NaCl

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41
Q

Name thiazide diuretics

A

Bendroflumethiazide
Metolazone
Chlortalidone

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42
Q

SEs of thiazide diuretics e.g. bendroflumethiazide

A 
low K+
low Na+
high calcium
high urate (gout) (as compete for the same transporter)
postural hypotension 
increased glucose and DM
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43
Q

Contraindications to thiazide diuretics

A

Gout
Refractory hypokalaemia
Severe renal failure

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44
Q

Interactions of thiazides

A

increase toxicity of digoxin and lithium

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45
Q

What are nifedipine and amlodipine? When are they used?

A

Dihydropyridine Calcium channel blockers

Used in treatment of HTN, angina, prinzmetals angina and raynauds

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46
Q

How does nifedipine work?

A 
Blockers of calcium channels mainly in arterial smooth muscle 
Cause vasodilatation (including of coronary arteries) (particularly of pre-capillary arterioles)
Decrease total peripheral resistance so increase sympathetic tone and therefore increase HR
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47
Q

What are side effects of amlodipine and nifedipine

A 
flushing
headache
ankle oedema (amlodipine)
dizziness
hypotension
gingival hypertrophy (nifedipine)
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48
Q

Contraindications to dihydropyridine CCBs?

A

cardiogenic shock
unstable angina
significant AS
within 1month of MI

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49
Q

What do dihydropyridine CCBs interact with?

A

alpha / beta blockers - > hypotension
grapefruit juice increases dose (p450 inhibitor)
rifampicin, CMZ and phenytoin decrease dose (p450 inducers)
nifedipine only - increases function of digoxin

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50
Q

What are diltiazem and verapamil

A

Non-dihydropyridine CCBs

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51
Q

How does diltiazem work?

A

Block calcium channels
Mainly cardiac effect
-ve inotrope
(verapamil also slows conduction at SA and AV node)
some activity at arterial SM (<dihydropyridines)

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52
Q

What are SEs of verapamil and diltiazem

A 
headache
flushing
ankle oedema
AV block
HF
Hypotension
constipation
gynacomastia (verapamil)
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53
Q

When are verapamil and diltiazem contraindicated?

A

HF (2nd/3rd degree AV block)

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54
Q

What do verapamil and dilitiazem interact with

A

Beta blockers - risk of AV block, HF and asystole
increase function of digoxin
function of verapamil increased by grapefruit juice or macrocodes (p450 inhibitors)
simvastatin - increased risk of myopathy

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55
Q

when are non-dihydropyridines used?

A

Angina,
HTN
arrhythmias (verapamil)

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56
Q

Clopidogrel

A

irreversible adenosine receptor antagonist

inhibits ADP-induced fibrinogen binding to GPIIb/IIIa

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57
Q

SEs clopidogrel

A 
bleeding
GI upset
dyspepsia / PUD
TTP (rare)
blood dyscrasias (rare)
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58
Q

When should clopidogrel not be used?

A

With warfarin

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59
Q

Amiodarone. MOA?

A

Class III - K+ channel blocker

Increases refractory period - increases QT interval

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60
Q

When is amiodarone used?

A

Ventricular and supra ventricular tachycardias and WPW syndrome.

BUT can cause arrhythmias (torsades de points)

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61
Q

Aspirin. MOA?

A

Irreversible non selective COX inhibitor
Prevents formation of thromboxane A2 and therefore decreases platelet adhesion and aggregation.

Relatively platelet specific at low doses 75mg-150mg

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62
Q

Side effects of aspirin?

A

Gastritis
Gastric ulceration
Bleeding
Bronchospasm

Rarer:
renal failure
gout
ototoxic in overdose: tinnitis

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63
Q

Contraindications to aspirin

A

<10ml/min
Pregnancy

Caution in asthma & uncontrolled hypertension

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64
Q

What does aspirin interact with?

A

Other anti-coagulants and anti-platelets -> bleeding

Increases function of sulphonylureas and methotrexate

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65
Q

When should aspirin be stopped before a surgery which may involve significant bleeding?

A

7 days

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66
Q

Digoxin. MOA?

A

Cardiac glycoside - bind to Na/K ATPase & cause build up of intracellular calcium
Anti-arrythmic agent
Increase contractility of myocytes

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67
Q

When is digoxin prescribed?

A

AF/flutter
SVT
(HF)

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68
Q

What are SEs of digoxin

A

Due to Toxicity:
Arrhythmias
Nausea
Xanthopsia (yellow tint)

Chronic SE:
gynaecomastia

“reverse tick” ECG - not a sign of toxicity

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69
Q

Contraindications to taking digoxin

A

Complete heart block
VF/VT
HOCM
SVTs secondary to WPW

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70
Q

What does digoxin interact with?

A

Digoxin function increased by:
CCB (esp verapamil)
Diuretics (loop / thiazide due to decreased K)
Amiodarone (halve digoxin dose)

Decreased digoxin absorption:
antacids
cholestyramine

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71
Q

Side effects of amiodarone

A

EYE - corneal microdeposits

Thyroid - hyper/hypo

Lung - pulmonary fibrosis

GI/Liver - increased LFTs, N/V

Neuro - peripheral neuropathy

Skin - photosensitivity, blue/grey discolouration, phlebitis (give centrally)

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72
Q

Side effects of methotrexate

A

Myelosuppression
Liver cirrhosis
Pneumonitis

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73
Q

Side effects of sulfasalazine

A

Rashes
Oligospermia (low sperm count)
Heinz body anaemia
stevens- Johnson syndrome

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74
Q

Side effects of leflunomide

A

Liver impairment
Interstitial lung disease
Hypertension

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75
Q

What is methotrexate ?

A

Antifolate (Inhibits dihydrofolate reductase and thymidylate synthesis)

Commonly used in rheumatoid arthritis

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76
Q

What is leflunomide

A

Dmard

Pyramiding synthesis inhibitor

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77
Q

What is hydroxychloroquine? What are it’s side effects?

A

Antimalarial (used in RA)

Retinopathy
Corneal deposits

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78
Q

What are the side effects of prednisolone?

A 
Cushingoid (centripetal weight gain, moon face, buffalo hump) 
Osteoporosis
Decreased glucose tolerance 
Hypertension 
Cataracts
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79
Q

What is a side effect of gold

A

Proteinuria

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80
Q

Side effects of penicillamine

A

Proteinuria

Exacerbation of myasthenia gravis

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81
Q

Ethanercept - TNF inhibitor

Side effects?

A

Demyelination

Reactivation of Tb

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82
Q

Infliximab (TNF mab) side effects?

A

Reactivation of Tb

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83
Q

Adalimumab (TNF mab) side effects

A

Reactivation of Tb

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84
Q

Rituximab - anti cd20 side effect?

A

Infusion reactions common

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85
Q

Dipyridamole. MOA?

A

Class I anti-arrhythmic
Phosphodiesterase inhibitor - increased cAMP inhibits platelet aggregation
Thromboxane A2 synthetase inhibitor

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86
Q

SE of dipyridamole?

A

Headache

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87
Q

What does dipyridamole interact with?

A

enhances effects of adenosine

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88
Q

When is dipyridamole used?

A

May be used with aspirin in secondary prevention of stroke

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89
Q

When is dipyridamole contraindicated?

A

Myasthenia gravis

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90
Q

How does bumetanide work?

A

Loop diuretic (like furosemide)
Inhibits Na/K/Cl transporter in ascending limb of loop of Henle
Increases NaCl excretion

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91
Q

SEs of loop diuretics?

A 
Low Na
Low K
Low Ca
Low Mg
High Urate
Postural hypotension
Tinnitus / deafness (rare)

(monitor U&Es)
(May add K+ sparing diuretic to decrease K loss)

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92
Q

What are contraindications to taking loop diuretics?

A

Refractory hypokalaemia

Anuric renal failure

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93
Q

What do loop diuretics interact with

A

Increase toxicity of:

  • digoxin (due to decreased K)
  • NSAIDs
  • Gentamicin
  • Li
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94
Q

Nicorandil. MOA?

A

K(ATP) channel activator & nitrate component
Arterial and venous dilator
Used as an anti-anginal in uncontrolled angina

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95
Q

SEs Nicorandil

A

Flushing
Headache
Dizziness
GI ulcers (rare)

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96
Q

When is nicorandil contraindicated

A

Cardiogenic shock

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97
Q

What does nicorandil interact with

A

Sildenafil (decreases BP)

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98
Q

GTN. MOA?

A

NO donor with rapid onset and short duration (30 mins)
Used for angina

cause release of nitric oxide in smooth muscle, increasing cGMP which leads to a fall in intracellular calcium levels

in angina they both dilate the coronary arteries and also reduce venous return which in turn reduces left ventricular work, reducing myocardial oxygen demand

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99
Q

Isosorbide mononitrate -MOA?

A

Long acting nitrate - used for angina

Is an active metabolite of ISDN
Mononitrate avoids unpredictable first pass metabolism of denitrate

Tolerance develops quickly: need 8h drug free period (usually at night)

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100
Q

SEs of nitrates?

A

Hypotension
Headache

syncope
dizziness
flushing
reflex tachycardia

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101
Q

CIs to nitrates

A 
Atrial stenosis and Mitral stenosis
Hypotension
Constrictive pericarditis
Tamponade
HOCM
Low Hb
Glaucoma (closed)
Hypovolaemia
Increased ICP
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102
Q

What do nitrates interact with?

A

sildenafil, tadakafil and vardenafil -> low BP

Decreased function of heparins if given IV

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103
Q

prothrombin complex concentrate- MOA

A

combination of blood clotting factors II, VII, IX and X, as well as protein C and S

prepared from fresh-frozen human blood plasma

used to reverse the effects of oral anticoagulation therapy (warfarin) when bleeding occurs

when INR >8

also used in deficiencies of clotting factors e.g. congenital, haemophilia, or liver disease

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104
Q

Spironolactone / eplerenone. MOA?

A

Aldosterone receptor antagonist
K+ sparing diuretic
Increase Na excretion
Decrease H and K excretion

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105
Q

Side effects of spironolactone

A

Increased K

Gynacomastia

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106
Q

Contraindications to spironolactone

A

increased K
Pregnancy
Addisons

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107
Q

Spironolactone interacts with which drugs?

A

Digoxin and lithium - increases their toxicity

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108
Q

Amiloride. MOA?

A

Typically used in combination with K+ wasting diuretics.
Block Na channels in collecting tubules
- increase Na excretion
- decrease K and H excretion

SE: include increased K+ and GI upset

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109
Q

Statins. MOA?

A 
Lipid lowering therapy
HMG-CoA reductase inhibitors - block the rate limiting step in cholesterol synthesis
- decrease hepatocyte cholesterol
- increase hepatic LDL receptors
- decrease LDL cholesterol
- increase HDL
- decrease triglycerides (mild)
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110
Q

SEs of statins

A

Myositis

  • stop if CK 5x ULN
  • can cause rhabdomyolysis & ATN

Deranged LFTs
GI upset

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111
Q

Contraindications to statins

A

Pregnancy ( contraception needed during use and for 1 month after)
L

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112
Q

When are statins indicated

A

any known CVD
DM (age >40)
10yr CVD risk >20%

AIM: TC<4mM

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113
Q

What do statins interact with

A

Increased risk of myositis with:

  • fibrates
  • macrolides
  • azoles
  • grapefruit juice
  • protease inhibitors
  • ciclosporin
  • nicotinic acid
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114
Q

What time of day should statins be taken? What should be monitored on statins?

A

LFTs and CK

Take nocturnally as increased cholesterol synthesis overnight

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115
Q

What are examples of alpha receptor blockers?

A

Alfuzosin
Doxazosin (alpha1)
Tamluzosin

(phenoxybenzamine and phentolamine are non selective alpha receptor blockers)

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116
Q

How does doxazocin work?

A

alpha 1 receptor blocker
systemic vasodilatation - antihypertensive
relaxation of internal urethral sphincter

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117
Q

Side effects of alpha blockers

A 
postural hypotension
dizziness
headache
urinary incontinence (esp women)
blurred vision
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118
Q

What do alpha blockers interact with?

A

diuretics
Beta blockers
CCBs

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119
Q

Phentolamine - what is it & what is it used for

A

Non selective alpha receptor blocker

SHort acting - used to control BP in phaeochromocytoma

120
Q

Phenoxybenzamine. MOA. USE?

A

Alpha receptor blocker
Long acting
Used to maintain alpha blockade in phaeochromocytoma once BP is controlled

121
Q

When are doxazosin and tamulosin used? MOA

A

Alpha 1 receptor blockers

used in treatment of benign prostatic hypertrophy

122
Q

Name cardioselective beta blockers

A

bisoprolol
atenolol
metoprolol

123
Q

name non-selective beta blockers

A

propranolol
carvedilol
sotalol
labetolol

124
Q

How do beta blockers work?

A

act via B1 receptors to decrease CO

  • decrease HR
  • decrease contractility
  • small decrease in BP: central effect due to decreased renin

Effects:
increase diastolic perfusion
decrease o2 demand
decrease afterload

125
Q

Side effects of beta blockers

A

Bronchospasm

Peripheral vasoconstriction - cold extremities - worsens Raynauds and peripheral vascular disease

Lethargy / fatigue
Nightmares

Metabolic - decrease HDL, increase triglycerides, increase risk of new onset DM

126
Q

What do beta blockers interact with

A

Verapamil and diltiazem - risk of AV block and decreased HR

Enhanced decreased BP with other anti-HTN drugs

Block symptoms of decreased glucose with insulin

127
Q

When is amiodarone prescribed

A

SVT
AF/flutter
pre-excited AF
ventricular arrhythmias (incl VF)

128
Q

When is amiodarone contraindicated

A

Thyroid disease
Sinus bradycardia
increased QT interval - causes torsades de pointes

129
Q

What does amiodarone interact with

A

Beta blockers and CCB - increase risk of heart block
Increased levels of digoxin, warfarin and phenytoin
Increase risk of ventricular arrhythmias with class III/IIa antiarrhythmics, TCAs, antipsychotics, eryhtromycin

130
Q

What is ipratropium. what does it do?

A

Short acting muscarinic antagonist
3-6hrs

bronchodilation
decreases mucus secretion

SE: dry mouth
Caution: with close angle glaucoma & prostatic hypertrophy

131
Q

What is tiotropium?

A

Long acting muscarinic antagonist
aka Spiriva

bronchodilatation
decreased mucus secretion

SE: dry mouth
Caution with closed angle glaucoma and prostatic hypertrophy

132
Q

Salbutamol

A

short acting beta agonist
act on bronchial B2 receptors
SM relaxation
decrease mucus secretion

133
Q

SE of salbutamol

A

Tachycardia
Tremor

low K+ in high doses with corticosteroids, loop/thiazide diuretics or theophylline

134
Q

Salmeterol

A

Long acting beta agonist

12-18 hrs

135
Q

Chloramphenamine

A

Antihistamine
Piriton

H1 receptor inverse agonist

136
Q

SE of chloramphenamine

A

Hypotension
arrhythmia (increase QT interval)
Drowsiness
Anti-AChM

137
Q

When is chloramphenamine contraindicated

A

severe hepatic disease

Use with caution in:
Long QT
BPH
Closed angle glaucoma

138
Q

Beclometasone

A

Inhaled corticosteroids
act over weeks to decrease inflammation
decrease cytokine production
decrease prostaglandin / leukotriene synthesis
decrease IgE secretion
decrease leukocytes recruitment
prevent long term decrease in lung function

139
Q

SE of inhaled corticosteroids

A

oral candidiasis

high doses may cause typical steroids SEs

140
Q

Budesonide

A

Pulmicort

Inhaled corticosteroids
act over weeks to decrease inflammation
decrease cytokine production
decrease prostaglandin / leukotriene synthesis
decrease IgE secretion
decrease leukocytes recruitment
prevent long term decrease in lung function

141
Q

Fluticasone

A

Inhaled corticosteroids
act over weeks to decrease inflammation
decrease cytokine production
decrease prostaglandin / leukotriene synthesis
decrease IgE secretion
decrease leukocytes recruitment
prevent long term decrease in lung function

142
Q

Symbicort

A

Budesonide (inhaled corticosteroid) and formoterol (long acting beta agonist)

143
Q

Seretide

A

fluticasone (inhaled corticosteroid) + salmeterol (long acting beta agonist)

144
Q

Nicotine replacement therapies

A

Nicotine patches, acuhalers, gum

Buproprion - decrease cravings (noradrenaline, dopamine reuptake inhibitor)
SE: increase risk of epileptic seizures if epileptic

145
Q

What are the main SEs of metformin

A

GI side effects

lactic acidosis

146
Q

What are the main SEs of glimepiride

A

Glimepiride is a sulphonylurea used in the treatment of diabetes.

SE: hypoglycaemic episodes
increased appetite and weight gain
SI ADH
liver dysfunction (cholestatic)
photosensitivity
peripheral neuropathy
147
Q

What are the SEs of pioglitazone

A

Pioglitazone is a glitazone used in the treatment of diabetes.

SE include: weight gain
fluid retention
liver dysfunction
fractures

148
Q

What are examples of atypical antipsychotics?

A

Olanzapine
Clozapine
Quetiapine
Risperidone

149
Q

What is quetiapine?

A

Atypical antipsychotic

Dopamine antagonists

150
Q

What are the side effects of olanzapine?

A

weight gain
DM
sedation

151
Q

What are the side effects of clozapine?

A

agranulocytosis
weight gain
DM

(atypical antipsychotic used in the treatement of refractory schizophrenia)

152
Q

What are the side effects of quetiapine

A

atypical antipsychotic - dopamine antagonist

SE: sedation

153
Q

What are the side effects of risperidone?

A

atypical antipsychotic - dopamine antagonist

SE: increased weight, increased prolactin

154
Q

Lithium. SEs:

A

Mood stabiliser

SEs: polyuria and polydipsia
nephrotoxic
GI upset
fine tremor
hypothyroidism

TOXICITY: coarse tremor, cerebellar signs, AKI, hyper-reflexia, coma

155
Q

Lithium interacts with?

A

NSAIDS, diuretics and ACEI/ARB increase the toxicity of lithium

156
Q

What are examples of benzodiazepines?

A 
chlordiazepoxide
diazepam
lorazepam
midazolam
temazepam
157
Q

How do benzodiazepines work?

A

Promote GABA binding to GABAa receptors

158
Q

SEs of chlordiazepoxide?

A

benzodiazepine SEs:
sedation
respiratory depression
withdrawal

159
Q

Levels of benzodiazepines increased by:

A

Antipsychotics
Azoles
Macrolides

160
Q

How would you treat a benzodiazepine overdose?

A

Flumazenil

161
Q

What are examples of typical antipsychotics

A

chlorpromazine
haldol
sulpiride
zuclopenthixol

(dopamine antagonists)

162
Q

Side effects of typical antipsychotics

A 
sedation
anti-AChM
EPSEs - extrapyramidal side effects
neuroleptic malignant syndrome
Increase QT
postural hypotension
increased prolactin
sexual dysfunction
increased weight
163
Q

Cocodamol. what is it?

A

Mix of paracetamol and codeine

Paracetamol = antipyretic & analgesic
Codeine = weak opioid (via mu receptor)
164
Q

Co-dydramol. what is it

A

Mix of dyhydrocodeine tartrate & paracetamol

Dyhydrocodeine = weak opioid

165
Q

What are side effects of opioids?

A 
CNS SEs:
Resp depression
sedation
n/v
euphoria
meiosis
anti-tussive
dependence
Non-CNS
constipation 
urinary retention
pruritis
bradycardia, hypotension

TREAT OVERDOSE WITH NALOXONE

decrease dose in renal impairment, hepatic impairment & elderly

166
Q

Gabapentin SEs:

A

MOA unknown

sedation
cerebellar function
dizziness
peripheral oedema

167
Q

What are examples of opioids

A 
Strong opioids:
morphine
fentanyl
pethidine
diamorphine
oxycodone
buprenorphine

weak opioids
dihydrocodeine
tramadol

168
Q

Examples of TCAs

A 
Amitriptylline
Nortroptyline
lofepramine
clomipramine
imipramine
doxepin
169
Q

How does amitriptyline work

A

TCA

inhibit 5HT and NA uptake

170
Q

SEs of TCAs?

A

alpha 1: postural hypotension, sedation

H1: drowsiness, weight gain

Anti-AChM

Arrhythmias - especially Heart block

171
Q

What do tricyclics interact with?

A

MAOIs -> hypertension and CNS excitation

Levels increased by SSRIs

Increased risk of arrhythmias with amiodarone

Lower seizure threshold - decrease effect of anti-epileptics

increase function of antipsychotics

172
Q

Contraindications to TCAs

A

Recent MI / arrythmia
Mania

Caution:
glaucoma
BPH

173
Q

What drugs cause urticaria

A

Immune: penicillins, cephalosporins

Non-immune: contrast, opiates, NSAIDs

174
Q

What drugs cause erythema nodosum

A

sulphonamides
penicillins
phenytoin
OCP

175
Q

What drugs cause erythema multiforme

A 
sulphonamides
NSAIDs
allopurinol
phenytoin
penicillin
176
Q

what drugs cause photosensitivity reactions to the skin

A

amiodarone
thiazides
sulfonylureas
doxycycline

177
Q

what drugs cause lupus like reactions to the skin

A

hydralazine
isoniazid
penicillamine

178
Q

What drugs cause fixed eruptions to the skin

A

erythromycin

sulphonamides

179
Q

Cyclizine. MOA

A

anti-emetic

H1 receptor antagonist

180
Q

Contraindications to cyclizine

A

severe HF

MOAIs (can increase cyclizine’s anti-AchM function)

181
Q

Indications for prescribing cyclizine?

A

Pnt on opioids

Vestibular

182
Q

Examples of D2 receptors antagonists?

A

Metoclopramide
Prochlorperazine
Domperidone

Anti-emetics

183
Q

Side effects of metoclopramide?

A

D2 receptor antagonist (like prochlorperazine and domperidone)

SEs:
Extrapyramidal SEs (EPSEs) - dystonias, oculogyric crisis

Drowsiness
Rash
allergy
Increased prolactin

184
Q

metoclopramine - interactions?

A

Increased risk of EPSEs with antipsychotics, TCAs and SSRIs

domperidone does not cross the BBB and therefore has less EPSEs than the others

185
Q

Indications for prochlorperazine?

A

And other D2-receptor antagonists used as anti-emetics

GI causes - esp GORD
Chemo
Morning after pill
Opiates
PD
Migraine
Vestibular
186
Q

Levodopa. MOA

A

Dopamine pro-drug

crosses BBB and converted into dopamine by dopa-decarboxylase

give with peripheral dopamine decarboxylase inhibitor e.g. carbidopa (co-careldopa) or benserezide (co-beneldopa)

short T1/2 therefore at least TDS

187
Q

Side effects of levodopa

A 
Dyskinesia
On-off phenomena
Psychosis
ABP decreased
Mouth dryness
Insomnia
N/V
EDS
188
Q

COntraindications to levodopa

A

glaucoma (closed)
MAOIs -> hypertensive crisis
Melanoma

189
Q

Interactions of levodopa

A

Function decreased by antipsychotics

Hypertensive crisis with non-selective MOAIs

Food affects absorption

190
Q

Synthetic dopamine agonists used in parkinsons disease?

A

ropinerole
rotigotine
pramipexole

191
Q

Selegiline

A

example of a selective MOA-B inhibitor used in parkinsons

rasagiline

prevent intraneuronal degradation of dopamine

Used alone to delay need for L-dopa. Adjunct to L-dopa to decrease end of dose effects

192
Q

Entacapone

A 
COMT inhibitor (like tolcapone) used in PD
Inhibit peripheral Da degradation

SEs: reddish-brown urine, GI, dyskinesias

193
Q

Ondansetron

A

5HT3 receptor antagonist
anti-emetic

used post-op or after chemo

194
Q

Interactions of ondansetron

A

Levels decreased by rifampicin, CBZ, phenytoin

Avoid with drugs that increase QT interval

195
Q

Phenytoin

A

Anti-epileptic
Na channel blocker
Use dependent
Inhibit action potential generation

196
Q

SEs phenytoin

A

Acute:
drowsiness
cerebellar symptoms - DANISH
rash

Chronic
gingival hypertrophy
hirsuitism & acne
decreased folate -> megaloblatstic anaemia
peripheral neuropathy
lymphadenopathy
Idiosyncratic
fever
rashes, incl toxic epidermal necrolysis
hepatitis
Dupuytren's contracture
aplastic anaemia
drug-induced lupus

Teratogenic
associated with cleft palate and congenital heart disease

197
Q

Phenytoin has many interactions as is a cytochrome P450 inducer. Contraindications?

A

Don’t give IV if cardiac dysrhythmias

Caution: DM, hypotension, pregnancy

198
Q

Sodium valproate. SEs

A 
Valproate
Appetite increases
Liver failure
Pancreatitis
Reversible hair loss
Oedema
Ataxia
Teratogenicity, Tremor, thrombocytopenia
Encephalopathy
199
Q

Sodium valproate

A

first line for primary generalised epilepsy
Cytochrome p450 inhibitor
Monitor FBC, LFTs

200
Q

Name SSRIs

A

Paroxetine
Citalopram
Fluoxetine
sertraline

201
Q

SEs SSRIs

A 
N/V
Insomnia
Headache
Sexual dysfunction
SIADH
Withdrawal effects
202
Q

Fluoxetine - interactions?

A

SSRI Interactions:
It is a p450 inhibitor so increases levels of TCAs, benzos, clozapine, haldol, cbz, phenytoin

SSRI+MOAI -> serotonin syndrome

increased risk of bleeding with aspirin

203
Q

Venlafaxine

A

SNRI

2nd line anti-depressant

204
Q

Zopliclone

A

used to treat insomnia

non-benzo

205
Q

Pioglitazone. What is it? how does it work?

A

Thiazolidinediones are a new class of agents used in the treatment of type 2 diabetes mellitus.

They are agonists to the PPAR-gamma receptor and reduce peripheral insulin resistance.

Rosiglitazone was withdrawn in 2010 following concerns about the cardiovascular side-effect profile.

206
Q

Gabapentin. MOA? SEs?

A

MOA unknown

SE: sedation, cerebellar dysfunction, dizziness and peripheral oedema

207
Q

What is the function of gabapentin affected by?

A

decreased by: antidepressants

antimalarials

208
Q

What is cephalexin

A

1st generation cephalosporin antibiotic- beta lactam Abx
Used for UTIs

Bactericidal - inhibit bacterial transpeptidase enzyme required for cell wall construction.

increasing generations have increasing activity against gram -ve organisms

209
Q

Cefuroxime

A

2nd generation cephalosporin

Bactericidal beta lactam abx - inhibit transpeptidase required for cell wall construction. Gram -ve activity

Used for Mod/Severe CAP, GI sepsis, Pre-op

210
Q

Cefotaxime / ceftriaxone

A

Cephalosporin - 3rd generation

Bactericidal
Inhibit bacterial transpeptidase enzyme. Required for cell wall construction.

Used in meningitis, epiglottis, gonorrhoea, SBP

211
Q

SEs cephalosporins?

A

1st gen- cephalexin
2nd gen - cefuroxime
3rd gen - cefotaxime, ceftriaxone

SE: GI upset

CI: hypersensitivity reactions

212
Q

Ciprofloxacin MOA. Use?

A

Fluroquinolone
Bactericidal - inhibit DNA synthesis. Inhibit topoisomerase II.

Broad spectrum
especially gram -ve GI infections: campylobacter, shigella, pseudomonas (esp in CF), prostatitis, PID, protozoa (giardia)

213
Q

SEs fluoroquinolones?

A

Ciprofloxacin, Moxifloxacin, levofloxacin

increased QT interval
GI upset
Tendonitis + rupture: e.g. achilles tendon rupture
reduced seizure threshold
photosensitivity

CI: pregnancy

214
Q

Interactions of fluoroquinolones

A

P450 inhibitor

Decreased absorption with antacids

215
Q

Cyclophosphamide. Adverse effects

A 
Acute myeloid leukaemia
Bladder Cancer
Haemorrhagic cystitis
Infertility
Bone marrow suppression
Alopecia

Used as an immunosuppressant - cancer treatment, glomerulonephritis / tubulointerstitial nephritis, autoimmune conditions

216
Q

Cyclophosphamide MOA

A

Metabolite (converted from pro-drug by ctyochrome p450 enzymes) phosphamide mustard forms cross links with DNA -> elimination of T cells

217
Q

Drugs to avoid in renal failure

A
  • antibiotics: tetracycline, nitrofurantoin
  • NSAIDs
  • lithium
  • metformin
218
Q

How to treat a TCA overdose

A

Management
IV bicarbonate may reduce the risk of seizures and arrhythmias in severe toxicity

arrhythmias: class 1a (e.g. Quinidine) and class Ic antiarrhythmics (e.g. Flecainide) are contraindicated as they prolong depolarisation. 
Class III drugs such as amiodarone should also be avoided as they prolong the QT interval. Response to lignocaine is variable

correction of acidosis is the first line in management of tricyclic induced arrhythmias
dialysis is ineffective in removing tricyclics

219
Q

Management of Lithium overdose

A

mild-moderate toxicity may respond to volume resuscitation with normal saline

haemodialysis may be needed in severe toxicity

sodium bicarbonate is sometimes used but there is limited evidence to support this. By increasing the alkalinity of the urine it promotes lithium excretion

220
Q

Rx warfarin overdose

A

Vit K

Prothrombin complex

221
Q

Rx heparin overdose

A

protamine sulphate

222
Q

Rx Beta blocker overdose

A

If bradycardic - atropine

If resistant - glucagon may be used

223
Q

Rx ethylene glycol

A

Fomepizole = first line
Ethanol
Haemodialysis in refractory cases

224
Q

Methanol poisoning treatment

A

Ethanol or fomepizole

Haemodialysis in refractory cases

225
Q

Rx organophosphate insecticides

A

atropine

the role of pralidoxime is still unclear - meta-analyses to date have failed to show any clear benefit

226
Q

Rx digoxin overdose

A

Digoxin specific antibody fragments

227
Q

Rx iron overdose

A

Desferrioxamine, a chelating agent

228
Q

Rx lead overdose

A

Dimercaprol, calcium edetate

229
Q

Rx cyanide overdose

A

Hydroxocobalamin; also combination of amyl nitrite, sodium nitrite, and sodium thiosulfate

Dicobalt edentate

230
Q

SEs sildenafil

A

PDE V inhibitor - impotence

SEs:
blue discolouration of vision
non-arteritic anterior ischaemic neuropathy
nasal congestion
flushing
gastrointestinal side-effects
headache
231
Q

Gentamicin. MOA

A

aminoglycoside - bacteriocidal (amino-acyl site of 30s subunit)

other examples of amino glycosides include amikacin, streptomycin, neomycin

232
Q

When is gentamicin used?

A

Used for gram negative sepsis
Neutropenic sepsis
Otitis externa

Anti-pseudomonal

233
Q

SEs Gentamicin

A

nephrotoxic

Ototoxic

234
Q

Toxicity of gentamicin affected by?

A 
Toxicity increased by:
furosemide
cephs
vanc
ciclosporin
235
Q

Carbapenams. MOA? Examples?

A

Imipenam
Meropenam
Ertapenam

Bacteriocidal - inhibit bacterial transpeptidase enzyme required for cell wall construction

V broad spectrum (gram -,+ and anaerobes & pseudomonas)

Imipenam is rapidly inactivated by the kidney and must be given with cilastatin which blocks its metabolism

236
Q

When are carbapenams used?

A

all gram + except MRSA
most gram -ves
neutropenic sepsis

237
Q

SE carbapenams

A

GI upset

238
Q

Examples of macrolide antibiotics

A

clarithromycin
erythromycin
azithromycin

Bacteriostatic (50s subunit)

239
Q

When is clarithromycin used?

A

penicillin allergies
atypical pneumonia
chlamydia
H.Pylori

240
Q

SEs macrolides?

A

Increased QT interval
Dry skin
cholestatic hepatitis
GI prokinetic action

241
Q

Interactions of macrolides

A 
p450 inhibitor (increased dose of warfarin)
Increased dose digoxin
242
Q

Metronidazole

A

Inhibits DNA synthesis

Used for anaerobes
GI sepsis
Aspiration pneumonia
AAC (antibiotic-assoc colitis)
H.Pylori
PID
Protozoa: Giardia
243
Q

SEs metronidazole

A

Metallic taste
GI upset
gynaecomastia
peripheral neuropathy

AVOID ALCOHOL - disulfiram-like reaction
as aldehyde dehydrogenase inhibitor

244
Q

amphotericin B. what is it? what is it used for

A

anti-fungal
interacts with ergosterol -> pore formation -> fungicidal

used for severe systemic fungal infections IV such as cryptococcal meningitis, pulmonary aspergillosis, systemic candidiasis

245
Q

SEs amphotericin B

A

nephrotoxic (monitor Cr)

IV reaction (after 1-3h) - fever, hypotension, n/v

(PO version is non-toxic)

246
Q

Fluconazole. MOA

A

anti-fungal
blocks ergosterol synthesis by inhibiting 14 alpha-demethylase -> decreased membrane fluidity

inhibits replication
prevents hyphae formation

broad spectrum

fungistatic

247
Q

When is fluconazole used

A

oral/vag/oesophagus candida
alternative to amphotericin B for systemic infections

(P450 inhibitor)

248
Q

nystatin

A

anti-fungal

interacts with ergosterol -> pore formation -> fungicidal

used for candidiasis: cutaneous, vaginal, mucosal, oesophageal

toxic if given IV

249
Q

Amoxicillin. MOA. USES

A

Inhibits bacterial transpeptidase enzyme required for cell wall construction

bactericidal

broad spectrum

USES: pneumococcus, listeria, E.coli, enterococci

250
Q

Co-amoxiclav

A

amoxicillin
clavulinic acid

used for severe CAP , UTIs

251
Q

Tazocin

A

piperacillin + tazobactam

severe HAP
neutropenic sepsis

252
Q

Flucloxicillin

A

MSSA

penicillinase-resistant

253
Q 
Penicillin V
Penicillin G (IV)
A

Streps
N.meningitides
syphilis

254
Q

SEs of penicillins

A

hypersensitivity reaction: rash, anaphylaxis

GI upset

mac pap rash with EBV

255
Q

Interactions of penicillins

A

may decrease dose of OCP

dose increased by probenecid

256
Q

trimethoprim

A

folate antagonist
bacteriostatic

Used for UTIs, PCP, toxoplasmosis

SE: blood dyscrasias, nephro and hepato-toxicity

257
Q

Vancomycin

A

glycopeptides
bactericidal
(inhibit cell wall synthesis)

used for aerobic and anaerobic Gm + 
MRSA
HAN
Infective endocarditis
Antibiotic-assoc colitis
258
Q

SE vancomycin

A

nephrotoxic
ototoxic (tinnitus, SNHL)
hypersensitivity rash
neutropenia

MUST MONITOR LEVELS

259
Q

Bleomycin SE

A

degrades preformed DNA

SE: lung fibrosis

260
Q

Doxorubicin. MOA? SE?

A

Stabilizes DNA-topoisomerase II complex inhibits DNA & RNA synthesis

SE:Cardiomyopathy

261
Q

Fluorouracil MOA? SE?

A

Pyrimidine analogue inducing cell cycle arrest and apoptosis by blocking thymidylate synthase (works during S phase)

SEs:
Myelosuppression
mucositis
dermatitis

262
Q

Vincristine / vinblastine MOA? SE?

A

Inhibits formation of microtubules

SE vincristine: Peripheral neuropathy (reversible) , paralytic ileus

SE vinblastine: myelosuppresion

263
Q

Cisplatin MOA? SE?

A

Causes cross-linking in DNA

SE:
Ototoxicity
peripheral neuropathy
hypomagnesaemia

264
Q

SE GTN spray?

A

Hypotension
Tachycardia
Headache
Flushing

Tolerance may develop

265
Q

Clozapine SE

A

agranulocytosis
neutropenia
reduced seizure threshold

FBC monitoring essential during treatment

266
Q

Osteoporosis drug causes

A

Heparin
Corticosteroids
Pioglitazone

267
Q

Warfarin SE

A

haemorrhage
teratogenic, although can be used in breast-feeding mothers
skin necrosis: when warfarin is first started biosynthesis of protein C is reduced. This results in a temporary procoagulant state after initially starting warfarin, normally avoided by concurrent heparin administration. Thrombosis may occur in venules leading to skin necrosis
purple toes

268
Q

Factors that potentiate warfarin

A

Factors that may potentiate warfarin
liver disease
P450 enzyme inhibitors, e.g.: amiodarone, ciprofloxacin
cranberry juice
drugs which displace warfarin from plasma albumin, e.g. NSAIDs
inhibit platelet function: NSAIDs

269
Q

Atoraquone. What is it?

A

Often combined with progaunil (malarone)

Anti-malarial
take 1-2days before travel and for 7 days after

270
Q

Atoraquone and Proguanil SE?

A

GI upset

271
Q

Chloroquine SE. CI?

A

Anti-malarial (take 1 wk before and 4 wks after)
Taken weekly

Headache

CI: epilepsy

272
Q

Doxycycline SE?

A

anti-malarial

Photosensitivity
Oesophagitis

273
Q

Mefloquine. SE? CI?

A

Aka Larium
Anti-malarial (take 2-3wks before and 4 wks after)

SE: dizziness
Neuropsychiatric disturbance

CI: epilepsy

274
Q

NSAIDs SE?

A 
Abnormal LFTs (raised bilirubin &ALT)
PUD
decreased renal function

CI: asthma

275
Q

Drug causes of pancreatitis

A 
azathioprine
ARVs
prednisolone
sulphasalazine
didanosine
bendroflumethiazide
furosemide
pentamidine
sodium valproate
276
Q

Ciclosporin SE?

A

Ciclosporin is an immunosuppressant which decreases clonal proliferation of T cells by reducing IL-2 release. It acts by binding to cyclophilin forming a complex which inhibits calcineurin, a phosphotase that activates various transcription factors in T cells

Adverse effects of ciclosporin (note how everything is increased - fluid, BP, K+, hair, gums, glucose)
nephrotoxicity
hepatotoxicity
fluid retention
hypertension
hyperkalaemia
hypertrichosis
gingival hyperplasia
tremor
impaired glucose tolerance
hyperlipidaemia
increased susceptibility to severe infection

Interestingly it is ‘virtually non-myelotoxic’.

277
Q

Ciclsporin indications

A 
following organ transplantation
rheumatoid arthritis
psoriasis (has a direct effect on keratinocytes as well as modulating T cell function)
ulcerative colitis
pure red cell aplasia
278
Q

What would you use to treat a patient who has taken an antiemetic and now presents with protruding tongue, spasm of jaw, uncontrolled facial grimacing and torticollis?

A

Benztropine

to treat an acute dystonic reaction to dopaminergic antagonists.
blocks striatal cholinergic receptors, leading to rebalancing of cholinergic and dopaminergic activity in the brain.

279
Q

Name 3 anti-protozoal drugs

A

artesunate
quinine
chloroquine

280
Q

Gliclazide

A

Sulphonylurea
Insulin secretagogues
Block hyperpolarising K+ channel on β cells
→ depolarisation and insulin release

Used in treatment of DM

281
Q

Examples of sulphonylureas

A

Gliclazide
tolbutamide
glipizide
Glibenclamide

282
Q

SEs sulphonylureas

A

Hypoglycaemia
Weight gain
GI upset
Headache

283
Q

Gliclazide excretion and interactions?

A

Renally excreted

fx ↑d by:

  • sulphonamides
  • trimethoprim
  • NSAIDs
  • warfarin
  • fibrates
284
Q

Metformin

A

biguanide

Insulin sensitizer

  • ↓ gluconeogenesis
  • ↑ peripheral glucose use
  • ↓ LDL and VLDL
285
Q

SE metformin

and CI?

A

GI upset
Lactic acidosis

Renally excreted
Caution in renal or
hepatic impairment

CI:
Contrast media
General anaesthesia
Recent MI

286
Q

Pioglitazone

A

Thiazolidinedione
Peripheral insulin sensitizer
PPAR gamma ligand (nuclear receptor
involved in glucose and lipid homeostasis)

287
Q

Pioglitazone SEs?

A

Thiazolidinedione

SE: Wt. gain
Fluid retention
Hepatotoxicity
May exacerbate HF
Bladder cancer
Fractures
288
Q

Nateglinide
Repaglinide

SE?

A

Meglitinides
Insulin secretagogues
Block hyperpolarising K+ channel

SE: hypoglycaemia

289
Q

Exenatide

Liraglutide

A

Insulin secretagogue
GLP-1 analogue
- ↑ insulin secretion and sensitisation

SC injection

290
Q

Sitagliptin

Vildagliptin

A

Insulin secretagogues
Dipeptidylpeptidase-4 inhibitor
DPP-4 breaks down endogenous GLP-1

291
Q

Acarbose

A

Intestinal α-glucosidase inhibitor
Delays carb absorption → ↓ post-prandial
blood glucose
Little effect on fasting glucose

SE:Flatulence
Loose stools/diarrhoea
Abdo pain / bloating
Hepatotoxicity (rare)

292
Q

Levothyroxine

A

In elderly pts. c¯ subclinical heart failure thyroxine can
ppt. acute worsening: palpitations, angina, MI
-> Introduce thyroxine gradually
 Excessive thyroxine → osteopaenia and AF

293
Q

Carbimazole SE?

A 
Used to treat hyperthyroidism
Thionamides
- thyroperoxidase inhibitors
- prevent iodination of tyrosine
- → ↓ T4/T3 synthesis
Carbimazole is a pro-drug
- converted to methimazole
SE:
Agranulocytosis
- often transient and benign
Hypersensitvity: rash, pruritis
hepatitis

Propythiouracil is reserved for those
intoleant of carbimazole due to risk of
hepatitis

294
Q

Ezetimibe MOA? SE?

A

Used in hypercholesteraemia
Decrease cholesterol absorption in the small intestine

SE: headache

295
Q

Fibrates MOA? SEs?

A

Agonist of PPAR-alpha therefore increases lipoprotein lipase expression

SEs: Myositis pruritis cholestasis

296
Q

nicotinic acid

A

decreases VLDL secretion

flushing
myositis

297
Q

Finasteride

A

Finasteride is an inhibitor of 5 alpha-reductase, an enzyme which metabolises testosterone into dihydrotestosterone

Indications
benign prostatic hyperplasia
male-pattern baldness

Adverse effects
impotence
decrease libido
ejaculation disorders
gynaecomastia and breast tenderness

Finasteride causes decreased levels of serum prostate specific antigen

F****** Pharmocology (2 decks)

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