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MBChB Phase 3 > Even Numbers > Flashcards

Even Numbers Flashcards

1
Q

Clopidogrel

Mechanism (3)

Indication (1)

Side effects (2)

PK and PD (1)

Patient info (2)

Haematological

A

-> Anti-platelet drug

Mechanism of action:

  1. Irreversibly blocks the ADP(adenosine diphosphate)-receptor on platelet cell membranes
  2. Consequently inhibits formation of Glycoprotein IIb/IIIa complex, required for platelet aggregation (as it is the receptor for fibrinogen)
  3. Decreased thrombus formation

Indication:
- Secondary prevention of thrombotic events

Side effects:

  1. Bleeding (1-10% of patients)
  2. Abdominal pain/ diarrhoea (1-10% of patients)

Important PK and PD:
- Avoid in liver failure!

Patient info:

  • may be advice to stop clopidogrel before surgical procedures
  • patients should not stop clopidogrel without consulting their doctor if they have an arterial stent in-situ
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2
Q

Unfractioned Heparin

Mechanism of action (4)

Indications (3)

Side effects (3)

PK/PD (6)

Patient info (2)

Haematological

A

-> Heparins

Mechanism of action:

  1. Enhances activity of antithrombin III
  2. Antithrombin III inhibits thrombin.
  3. Heparins also inhibit multiple other factors of the coagulation cascade
  4. This produces its anticoagulant effect

Indications:

  1. Treatment and prophylaxis of thromboembolic diseases, including induction of vit. K antagonists
  2. Renal dialysis (Haemodialysis)
  3. Acute Coronary Syndrome treatment

Side effects:

  1. Bleeding ( Major haemorrhage risk can be as high as 3.5%)
  2. Heparin-induced thrombocytopenia
  3. Osteoporosis

PK/PD:

  1. Administered by continuous intravenous infusion or subcutaneous injections
  2. Non-linear relationship -> needs TDM (therapeutic drug monitoring)
  3. Effects monitored using activated partial thromboplastin time (aPTT)
  4. Can be reversed with protamine
  5. Unfractioned heparin has a shorter duration of action than LMW Heparin
  6. Because of 4 & 5 used in preference to LMW Heparin, in selected patients,(e.g. peri-operatively)

Patient Info:

  • Risk of bleeding
  • Regular blood monitoring is required
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3
Q

Vit. K Antagonist

Mechanism of action (3)

Indication (2)

Side effects (3)

PK/ PD (5)

Patient info (3)

Haematological

A

-> Warfarin

Mechanizm of action:

  1. Inhibits vit K epoxide reductase
  2. Prevents recycling of vit. K to reduced form after carboxylation of coagulation factors II, VII, IX, and X
  3. Prevents thrombus formation

Indications:

  1. Treatment of venous thromboembolism
  2. Thromboprophylaxis in: AF/ metallic heart valves/ cardiomyopathy

Side effects:

  1. Bleeding
  2. Warfarin necrosis
  3. Osteoporosis

PK/PD:

  1. There are numerous drug interactions/ food interactions
  2. Reversal by giving vit. K
  3. Polymorphism in key metabolizing enzymes (VKORC1 and CYP2C9)
  4. Needs therapeutic drug monitoring and monitored loading regimen
  5. Monitored with INR and dose adjusted according to indication

Patient info:

  1. Need for compliance/ attendance at visits for monitoring
  2. Care needed with alcohol
  3. Must inform doctor before starting new drugs - avoid over the counter aspirin preparations
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4
Q

Factor Xa Antagonists

Mech of A (2)

Indications (2)

Side effects (2)

PK PD (3)

Patient Info (1)

Haematological

A

-> Rivaroxaban

Mechanism of action:

  1. Inhibits conversion of prothrombin to thrombin, reducing concentrations of thrombin in the blood
  2. This inhibits the formation of fibrin clots

Indication:

  1. Treatment and Prophylaxis of venous thromboembolism (especially post-operative)
  2. Thromboprophylaxis in non-valvular AF

Side effects:

  1. Bleeding
  2. Nausea

PK PD:

  1. Predictable drug interactions (metabolized via CYP 450, inc CYP 3A4)
  2. No need for therapeutic monitoring
  3. Currently no available antidote

Patient info:
1.Risk of bleeding

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5
Q

Cardioselective Beta-blockers

Mechanism of action (5)

Indication (4)

Side effects (7)

PK/PD (3)

Patient info (2)

Cardiovascular

A

-> Bisoprolol, Atenolol

Mechanism of action:

  1. Cardioselective beta-1- adrenoreceptor antagonist
  2. Preferentially blocks the beta-1 receptors in cardiac and renal tissue
  3. Inhibits sympathetic stimulation of the heart and renal vasculature
  4. Blockade of the sino-atrial node reduces heart rate ( negative chronotropic effect) and blockade of receptors in the myocardium depresses cardiac contractility (negative inotropic effect)
  5. Additionally, blockade of beta-1 adrenoceptors in renal tissue inhibits the release of renin, depressing the vasoconstriction effects of the renin-angiotensin-aldosterone system

Indication:

  1. Hypertension
  2. Angina
  3. Rate-control in atrial fibrillation
  4. Carvedilol or Bisoprolol may be used as part of supportive therapy for mild/ moderate heart failure

Side effects:

  1. Bradycardia
  2. Hypotension
  3. Bronchospasm
  4. Fatigue (up to 10%)
  5. Cold extremities
  6. Sleep disturbances
  7. Loss of hypoglycemic awareness

PK/PD:

  1. Avoid higher doses and use with caution in patients with asthmatic and COPD- risk of bronchospasm
  2. Avoid in patients with history of frequent hypoglycaaemia
  3. Do not combine Beta-blockers with rate-limiting Ca2+ Channel Blockers (Verapamil/Diltiazem) in anti-hypertensive therapy, due to risk of heart- block

Patient info:

  1. Compliance is important- patients may stop beta-blockers if they do not feel any better; remind them that hypertension is symptomatic but nonetheless a dangerous risk factor that needs to be controlled
  2. Fatigue and cold extremities are common side-effects
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6
Q

ACE inhibitors

Mechanism of action (2)

Indication (4)

Side effects (5)

PK/PD (1)

Patient info (2)

Cardiovascular

A

-> Ramipril, Enalapril, Lisinopril, Perindopril

Mechanism of action:

  1. Inhibits conversion of Angiotensin I to Angiotensin II (a more potent systemic vascoconstriction)
  2. This action subsequently inhibits Aldosterone release from the adrenal cortex, depressing renal sodium and fluid retention, thereby decreasing blood volume

Indications:

  1. Hypertension
  2. HF
  3. Nephropathy
  4. Prevention of Cardiovascular events in high risk patients

Side effects:

  1. Dry cough (10 % of patients)
  2. Hypotension
  3. Hyperkalaemia ( high potassium)
  4. Renal impairment
  5. Angioedema

PK/PD:
1. Adverse drug reactions are higher in patients with: high-dose diuretic therapy/ Hypovolaemia/ Hyponatraemia/ Hypotension/ Unstable HF/ Retovascular disease

Patient info:

  1. Blood test required at 1-2 weeks to check electrolyte balance
  2. Dry cough is common side-effect
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7
Q

Rate limiting Calcium Channel Blockers

Mechanism of action (4)

Indications (3)

Side effects (2; 4)

PK/PD (3)

Patient info (3)

Cardiovascular

A

-> Varapamil; Diltiazem

Mechanism of action:

  1. Prevent cellular entry of Ca2+ by blocking L-type calcium channels
  2. Myocardial and smooth muscle contractility depressed. Cardiac contractility will be reduced.
  3. Dilate coronary blood vessels and reduce afterload
  4. Antidysrhythmic actions due to prolonged atrioventricular node conduction- depresses heart rate

Indications:

  1. Supraventricular arrhythmias
  2. Treatment of angina
  3. Hypertension

Side effects:
Verapamil
1. Constipation (up to 11.7%)
2. Flushing/ Headache/ Dizziness/ Hypotension ( up to 2.5%)

Diltiazem

  1. GI disturbances (up to 6%)
  2. Bradycardia (up to 3.6%)
  3. Peripheral oedema (up to 15%)
  4. Dizziness/ Headache/ Hypotension (is to 4.3%)

PK/PD:

  1. Contra-indicated in heart failure and left ventricular dysfunction due to potent negative inotropy
  2. Avoid in bradycardia and hypotension
  3. Do not use with beta-blockers

Patient information:

  1. Constipation is a common side effect with Verapamil
  2. Ankle swelling is a common side effect with Diltiazem hot weather making it worse
  3. Compliance is important- patients may stop calcium-channel blockers if they do not feel any better. Remind them that hypertension is symptomatic but nonetheless a dangerous risk factor that needs controlled
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8
Q

HMG CoA Reductase Inhibitors

Mechanism of action (5)

Indications (2)

Side effects (4)

Patient info (2)

Other (1)

Cardiovascular

A

->Simvastatin; Atorvastatin; Pravastatin

Mechanism of action:

  1. Competitively inhibits HMG CoA Reductase; the rate-determining enzyme in the mevalonate pathway synthesis of cholesterol
  2. This causes an increase in LDL- receptor expression, on the surface of hepatocytes
  3. Increases hepatic uptake of cholesterol, reducing plasma cholesterol levels
  4. Reduces development of atherosclerotic plaques
  5. Statins may have additional pleotropic effects

Indications:

  1. Familial hyper cholesterolaemia
  2. Prevention of cardiovascular events in high-risk patients

Side effects:

  1. Myalgia (5-7%)
  2. Myopathy ( with creatine kinase elevation) and rhabdomyolysis are rare
  3. GI disturbances (Varied symptoms; up to 6%)
  4. Liver abnormalities- deranged LFTs

PK/PD:
1. Myalgia and Rhabdomyolysis are dose- related, begin with low dose, especially in patients with previous side-effects

Patient info:

  1. . Report any unexpected muscle pains to their GP, who will check a creatine kinase blood level
  2. Diarrhoea and abdominal pain may be present initially
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9
Q

Anti-arrhythmic drugs

Mechanism of action (3)

Indications (1)

Side effects (7)

PK/PD (3)

Patient info (3)

Cardiovascular

A

-> Amiodarone

Mechanism of action:

  1. Blocks cardiac K+ channels, prolonging repolarisation of the cardiac action potential
  2. Restores regular sinus rhythm
  3. Slows atrioventricular nodal conduction

Indications:
1. Supraventricular/ventricular arrhythmias

Side effects:

  1. Photosensitivity skin reactions (up to 75%)
  2. Hypersensitivity reactions
  3. Hyper/ Hypothyroidism (high iodine content)
  4. Pulmonary fibrosis
  5. Corneal deposits (a lot)
  6. Neurological disturbances
  7. GI disturbances/ Hepatitis

PK/PD:

  1. Very long half-life, once daily dosing, can take weeks/months to achieve steady state amidarone-plasma concentrations
  2. Thyroid function tests should be performed before treatment and every 6 months or when symptomatic
  3. LFTs should be taken during treatment

Patient info:

  1. Need good compliance and attendance
  2. Avoid sun exposure, wear protective clothing
  3. Report presence of rush
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10
Q

Beta-lactams -> Cephalosporins

Mech (5)

Indications (1)

Side effects (3)

PK/PD (2)

Patient info (2)

Anti-infectives

A

-> Ceftriaxone, Cephalexin

Mechanism of action:

  1. Attaches to penicillin-binding-proteins on forming bacterial cell walls
  2. This inhibits the transpeptidase enzyme which cross links the bacterial cell wall
  3. Failure to cross-link induces bacterial cel autolysis
  4. Less susceptible to beta-lactamases than penicillins
  5. Provides both gram-positive an gram- negative cover

Indications:
1. Serious infection: septicaemia/ pneumonia/ meningitis

Side effects:

  1. Hypersensitivity reactions ( Low cross- reactivity in patients with true penicillin allergy- can be as low as 3-7%)
  2. Antibiotic-associated C. Difficult diarrhoea
  3. Liver function impairment

PK/PD:

  1. Renal excretion
  2. Longer half-life, needs to be given once daily

Patient info:

  1. Diarrhoea is a common side effect
  2. Report any incidence of a rash after use - Risk of hypersensitivity reactions
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11
Q

Aminoglycosides

Mech of action (3)

Indications (2)

Side effects (3)

PK/PD (4)

Patient info (2)

Anti-infectives

A

-> Gentamicin

Mechanism of action:

  1. Binds to 30s ribosomal subunit, inhibiting protein synthesis, inducing a prolonged post-antibiotic bacteriostatic effect
  2. Additionally, bactericidal action on bacterial cell wall results in rapid killing early in dosing interval and is prominent at high doses
  3. Also provides a synergic effect when used alongside other antibiotics (such as flucloxacillin or vancomycin in trap-positive infections)

Indications:

  1. Severe gram-negative infections (such as biliary tract infection, pyelonephritis, hospital-acquired pneumonia)
  2. Some severe gram-positive infection (such as soft tissue infection and endocarditis)

Side effects:

  1. Nephrotoxicity (2-10% patients affected)
  2. Ototoxicity
  3. Side -effects related to prolonged exposure to high-drug concentrations

PK/PD:

  1. Give high dose to take advantage of rapid killing
  2. Leave long dosing interval to minimize toxicity
  3. Measure trough level to ensure gentamicin is not accumulating and only prescribe further doses once this is confirmed
  4. Try to limit use to approx 3 days to minimize risk of side-effects

Patient info:

  1. Ask patients to report any change to their hearing
  2. Risk of kidney damage so monitoring of drug levels and renal function tests are required
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12
Q

Macrolides

Mech of action (2)

Indications (6)

Side effects (4)

PK/PD (2)

Patient info (3)

Anti-infectives

A

-> Clarithromycin, Erythromycin

Bacteriostaic and bacteriocidal

Mechanism of action:

  1. Binds to 50s ribosomal subunit
  2. Inhibits bacterial protein synthesis

Indications:

  1. Atypical organisms causing pneumonia/ Severe community acquired pneumonia
  2. Severe campylobacter infection
  3. Mild/ moderate skin and soft-tissue infection
  4. Otitis media
  5. Lyme disease
  6. Helicobacter pylori eradication therapy

Side effects:

  1. Diarrhoea
  2. Vomiting
  3. QT wave prolongation
  4. Ototoxicity with long-term use

PK/PD:

  1. Uses hepatic enzyme Cytochrome P450 pathway
  2. Can interact with all drugs using this pathway, especially Simvastatin, Atorvastatin and Warfarin

Patient info:

  1. Risk of diarrhoea
  2. Senses of smell and taste may be disturbed during therapy
  3. Tooth and tongue discoloration may occur during therapy
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13
Q

Anti-virals

Mech of action (2)

Indication (2)

Side effects (3)

PK/PD (3)

Patient info (1)

Other (1)

Anti-infectives

A

-> Aciclovir

Mechanism of action:

  1. A guanosine derivative, converted to triphosphate by infected host cells
  2. Aciclovir triphosphate then inhibits DNA polymerase, terminating the nucleotide chain and inhibiting viral DNA replication.

Indications:

  1. Herpes simplex infection
  2. Varicella zoster infection

Side effects:

  1. Nausea
  2. Vomiting
  3. Local inflammation at infusion site (IV only)

PK/PD:

  1. Can be given orally, intravenously or topically
  2. Penetrates well into the CSF with CSF concentrations being 50% concentration of that of plasma
  3. Excreted by the kidneys so dose adjustment is needed in renal impairment

Patient info:
1. Multiple/ repeat doses may be required in Immunosuppression patients

Other:
1. Type of infection/recurrent infection may prompt HIV testing

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14
Q

Beta- Adrenergic Bronchodilators

Mech of action (4)

Indications (2)

Side effects (4)

PK/PD (1)

Patient info (3)

Respiratory

A

-> Salmeterol

Mechanism of action:

  1. Long-acting Beta-2 adrenoceptor agonist (LABA)
  2. Relaxes bronchial smooth muscle, inducing bronchodilation
  3. Inhibit pro-inflammatory cytokine release from mast cells and TNF-a release from monocytes, reducing airway inflammation
  4. Increase mucus clearance from the airways by stimulating cilia action

Indications:

  1. Asthma
  2. COPD

Side effects:

  1. Tremor
  2. tachycardia/ cardiac dysrhythmia
  3. Headache
  4. Sleep disturbances

PK/PD:
1. Not to be commenced in patients with rapidly deteriorating asthma- slower onset of action than SABA’s

Patient info:

  1. Report any deterioration in symptoms following initiation of LABA
  2. Do not exceed stated dose
  3. Seek medical advice when stated dose fails to control symptoms
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15
Q

Inhaled Corticosteroids

Mech of action (3)

Indications (2)

Side effects (3)

PK/PD (2)

Patient info (2)

Respiratory

A

-> Beclomethasone
Some inhaled preparations used in COPD and asthma contain both inhaled steroids and long acting bronchodilators (eg Seretide and Symbicort)

Mechanism of action:

  1. Anti-inflammatory effect on the airways
  2. Decrease formation of pro-inflammatory cytokines
  3. Up-regulates beta-2-adrenoreceptors in airways

Indications:

  1. Treatment of CODP
  2. Treatment of asthma

Side effects:

  1. Oral Candiditis (thrush)
  2. Adrenal suppression
  3. Osteoporosis

PK/PD:

  1. Takes several weeks to months for full effect of therapy
  2. Spacer devices can reduce risk of thrush and improve drug delivery

Patient info:

  1. If on higher dose, carry a steroid card
  2. Increase dose during periods of illness
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16
Q

Dopamine precursor

Mech (3)

Indication (1)

Side effects (5)

PK/PD (4)

Patient info (3)

Neurology/Psychiatry

A

-> Levodopa

Mechanism of action:

  1. Pro-drug
  2. Crosses the blood brain barrier and is converted to dopamine
  3. Striata dopaminergic neurotransmission increased

Indication:
1. Parkinson’s Disease

Side effects:

  1. Dyskinesia
  2. Compulsive disorders
  3. Hallucinations
  4. Nausea
  5. GI upset

PK/PD:

  1. Converted to dopamine in peripheries (which can cause the meteor side effects)
  2. Given with a dopamine decarboxylase inhibitor or COMT inhibitor to reduce these effects
  3. Short half-life 50 to 90 mins
  4. Rapidly absorbed from the proximal small intestine via the large neutral amino acid (LNAA) transport carrier system

Patient info:

  1. Dyskinesia common
  2. Reduced efficacy over time
  3. Avoid abrupt withdrawal
17
Q

Catechol-o-methyl transferase inhibitor

Mechanism (2)

Indications (1)

Side effects (6)

PK/PD (2)

Patient info (3)

Neurology/ psychiatry

A

-> Entacapone

Mechanism of action:

  1. Prevents the peripheral breakdown of levodopa by inhibiting COMT (COMT converts L-DOPA into 3-method you-4-hydroxycarbamide-L-phenylalanine (3-OMD) 30 OMD does not cross the BBB
  2. More levodopa reaches the brain

Indications:
1. Parkinson’s Disease in conjunction with L-DOPA and dopamine decarboxylase inhibitor

Side effects:

  1. Dyskinesia (common up to 27%)
  2. Nausea (11%)
  3. Abdominal pain
  4. Vomiting
  5. Dry mouth
  6. Dizziness

PK/PD:

  1. Rapidly absorbed
  2. Levodopa dose may need to be reduced by 10-30% when given with Entacapone

Patient info:

  1. Urine may turn brown- normal
  2. Could become lightheaded/ dizzy while doing daily activities
  3. Avoid abrupt withdrawal
18
Q

Anti- Epileptic drugs

Mechanism (3)

Indication (3)

Side effects (8)

PK/PD (3)

Patient info (4)

A

-> Sodium Valproate

Mechanism of action:

  1. Weak sodium ion channel blocker
  2. Inhibitor of GABA degrading enzymes
  3. Increased GABA stops action potential

Indications:

  1. Epilepsy
  2. Bipolar disorder
  3. Depression

Side effects:

  1. Nausea
  2. Diarrhoea
  3. Gastric irritation
  4. Weight gain
  5. Hyponatraemia
  6. Behavioral disturbances (less common <10%)
  7. Confusion (less common <10%)
  8. Stevens-Johnson Syndrome (rare <0.1%)

PK/PD:

  1. Enzyme inhibitor of cytochrome P450
  2. Rapid absorption from GI tract- varies with formulation administered (liquid, solid, powder) and when administered (post- prendial or fasting)
  3. Can cause interactions with other anti-epileptic drugs

Patient info:

  1. Avoid alcohol
  2. Take with food
  3. Do not take with milk
  4. Lover function test must be monitored before and during the initial 6 months
19
Q

Anti- Epileptic drugs
Lamotrigine

Mechanism (4)

Indications (2)

Side effects (8)

PK/PD (1)

Patient info (2)

Neurology/ Psychiatry

A

-> Lamotrigrine

Mechanism of action:

  1. Varied mechanism of action
  2. Inhibits voltage- gated Na+ channels and/or Ca2+ channels
  3. Acts on pre-synaptic neuronal membrane
  4. Reduces action potential and excitatory signals

Indications:

  1. Epilepsy used for both partial and generalised seizures
  2. Depressive episodes associated with bipolar disorder

Side effects:

  1. Nausea
  2. Vomiting
  3. Diarrhoea
  4. Tremor
  5. Insomnia
  6. Blurred vision
  7. Aggression
  8. Skin reactions including Stevens-Johnson syndrome and toxic epidermal necrosis is (rarely)

PK/PD:
1. Half-life doubles in chronic renal impairment so dose adjustment is required

Patient info:

  1. Take without regard to meals
  2. Seek medical advice if any rash or sign/symptoms of hypersensitivity
20
Q

Selective Serotonin Reuptake Ihibitors (SSRIs)

Mechanism (2)

Indications (3)

Side effects (7)

PK/PD (2)

Patient info (3)

Neurology/ Psychiatry

A

-> Citalopram, Fluoxetine, Paroxetine, Escitalopram, Sertraline

Mechanism of action:

  1. Inhibition of reuptake of serotonin at the serotonin reuptake pump of the synaptic cleft
  2. Increases serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors

Indications:

  1. Depression
  2. Bulimia
  3. Obsessive Compulsive Disorder

Side effects:

  1. Dry mouth
  2. Nausea
  3. Insomnia
  4. Anxiety
  5. Decreased libido
  6. Seizures (rare)
  7. Dyskinesia (rare)

PK/PD:

  1. SSRIs bind with less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs. This leads to fewer side effects
  2. Less dangerous in overdose than tricyclic antidepressant drugs

Patient info:

  1. Be wary with alcohol- toxicity possible
  2. Improvement in depressive symptoms may take several weeks to occur
  3. Abrupt discontinuation from SSRIs may cause withdrawal symptoms (fatigue, tremor, sweating)
21
Q

Anti-psychotic drugs

Mechanism of action (4)

Indications (5)

Side effects (3)

PK/PD (1)

Patient info (2)

Neurology/ Psychiatry

A
  • > First generation: act non-selectively on D1-like and D2-like receptors (Haloperidol, Chlorpromazine)
  • > Atypical anti-psychotics: varying effect on dopamine and serotonin receptors (Olanzapine, Clozapine)

Mechanism of action:

  1. Block dopamine receptors
  2. Action on Mesolithic and nigrostriatal parts of brain
  3. Also have anti-histaminergic and anti-cholinergic effects
  4. These effects reduce positive symptoms of schizophrenia and can cause sedation and provide anti-emetic activity

Indications:

  1. Schizophrenia
  2. Mania
  3. Delusions, hallucinations
  4. Behavioral problems
  5. Anti-emetic (Haloperidol)

Side effects:

  1. Sedation (anti-histaminergic effects)
  2. Postural hypotension, tachycardia (anti-adrenergic effect)
  3. Urinary retention, dry mouth, blurry vision (anti-cholinergic)

PK/PD:
1. Have effects on numerous receptor systems within the central nervous system

Patient info:

  1. Symptoms may not always disappear while on medication
  2. Dosage may have to be increased if no improvement after a few weeks
22
Q

Corticosteroids (Glucocorticoids)

Mechanism of action (3)

Indications (4)

Side effects (11)

PK/PD (2)

Patient info (6)

Other (3)

Immuno-modulators

A 
Oral preparations (prednisolone, hydrocortisone dexamethasone)
Topical preparations (hydrocortisone, betamethasone, clobetasone)
Parenteral preparations (methyprednisolone, hydrocortisone, triamcinolone)

Mechanism of action:
1. Bind to glucocorticoid receptors
2. The causes up-regulation of a variety of anti-inflammatory mediators and down regulation of pro-inflammatory mediators
3. Provides immunosuppression
Also have a metabolic effect including increased gluconeogenesis

Indications:

  1. Replacement therapy in adrenal insufficiency
  2. Post-transplantation immunosuppression
  3. Treatment of exacerbations of a variety of inflammatory conditions (incl. eczema, RA, IBD and multiple sclerosis)
  4. Treatment of acute asthma

Side effects:

  1. Sleep disturbance
  2. Mood disturbance/ psychosis
  3. Hyperglycemia
  4. Immunodeficiency
  5. Easy bruising
  6. Moon-faced
  7. Increased abdominal fat
  8. Glaucoma
  9. Striae
  10. Hypertension
  11. Gastric irritation

PK/PD:

  1. A variety of different preparations are available
  2. Drugs have differing degrees of glucocorticoid and mineralocorticoid activity

Patient info:

  1. Avoid alcohol and caffeine
  2. Take with food to avoid gastric irritation
  3. Don’t stop abruptly
  4. Always tell doctors that are on prednisolone
  5. Carry steroid card
  6. Take a higher dose when ill

Other:

  1. Corticosteroids refer to both glucocorticoids or mineralocorticoid
  2. Glucocorticoids are different from mineralocorticoids by their receptors, target cells and function
  3. Different corticosteroid have differing glucocorticoid or mineralocorticoid activity

Prednisolone: predominant glucocorticoid activity, low mineralocorticoid act
Betamethasone: Potent glucocorticoid, no mineralocorticoid
Hydrocortisone: good glucocorticoid and mineralocorticoid act
Dexamethasone: potent potent glucocorticoid act minimal to no mineralocorticoid
Fludrocortisone: mild to moderate glucocorticoid, potent mineralocorticoid act

Functions of mineralocorticoids: increased resorption of water, increased res portion of sodium, increased renal excretion of potassium

23
Q

Immunosuppressant drugs

Mech of action (3)

Indications (4)

Side effects (8)

PK/PD (4)

Patient info (2)

Immuno- modulators

A

-> Methotrexate, Azathioprine, Mercaptopurine

Mech:

  1. Disrupt DNA synthesis
  2. Azathioprine: blocks purine synthesis mainly in lymphocytes
  3. Methotrexate: stops the action of the enzyme dihydrofolate needed for production of DNA

Indications:

  1. Post transplantation immunosuppression
  2. IBD
  3. Renal vasculitis
  4. Paediatric leukaemia (methotrexate is used)

Side effects:

  1. Bone marrow suppression (leucopenia)
  2. Risk of infection
  3. Nephrotoxicity
  4. Hepatotoxicity
  5. Seizures
  6. GI upset
  7. Mucosal ulceration
  8. Alopecia

PK/PD:

  1. Do not cross brain blood barrier
  2. Undergo hepatic metabolism
  3. Oral absorption is dose dependent
  4. Patients with low levels of thiopurine methyltransferase activity are more prone to Azathioprine and mercaptopurine related marrow suppression

Patient info:

  1. Limit caffeine intake
  2. Take without regard to leans
24
Q

H2 Receptor Antagonists

Mech of action (3)

Indications (3)

Side effects (5)

PK/PD (1)

Patient info (2)

Gastrointestinal

A

-> Ranitifdine, Cimetidine, Famotadine, Nizatidine

Mech of action:

  1. Histamine binds to H2 receptors on gastric parietal cells stimulating gastric acid secretion
  2. Drugs antagonist the effect of histamine at these H2 receptors
  3. Reduced cAMP and hence reduced activity of H+/K+ ATPase pump

Indications:

  1. Peptic ulcer
  2. Gastro-esophageal reflux disease
  3. Collin get- Ellison syndrome

Side effects:

  1. Headache
  2. Dizziness
  3. Diarrhoea
  4. Reduced B12 absorption
  5. Gynaecomastia

PK/PD:
1. Cimetidine is an inhibitor of cytochrome P450 enzymes

Patient info:

  1. Avoid high protein diet
  2. Take without regard to meals
25
Q

Anti-emetic drugs

Mech of action (3)

Indications (4)

Side effects (3)

PK/PD (1)

Patient info (3)

Other

GI

A

-> Cyclizine

Mechanism of action:

  1. Histamine H1 receptor antagonist
  2. Acts on vomiting center in the medullary region
  3. Mild anti-cholinergic and anti-muscarinic effect

Indications:

  1. Nausea and vomiting
  2. Motion sickness
  3. Vertigo and dizziness
  4. Prophylaxis alongside chemotherapy and opiate analgesic use

Side effects:

  1. Headache
  2. Sedation
  3. Diarrhoea

PK/PD:
1. It can also be a central nervous system depressant

Patient info:

  1. Avoid alcohol
  2. Food may reduce irritation
  3. Take without regard to meals

Other:
Many types of anti-emetics!
GO TO THE DOCUMENT

26
Q

Anti-emetic drugs

Mechanism of action (3)

Indications (2)

Side effects (4)

PK/PD (4)

Patient info (2)

Other (2)

GI

A

-> Prochlorperazine

Mechanism of action:

  1. Penothiazine anti-psychotic drug used as an anti-emetic
  2. Dopamine (D2) receptor antagonist
  3. Causes increased dopamine turnover (in mesolimbic and chemoreceptors trigger zone)

Indications:

  1. Nausea and vomiting
  2. Caused as an adjunct in some psychotic disorders

Side effects:

  1. Dry mouth
  2. Tachycardia
  3. Restless
  4. Drowsiness

PK/PD:

  1. Anticholinergics and alpha-adrenergic receptors antagonism occurs leading to sedation, muscle relaxation and hypotension
  2. The dose differs substantially when given parenteral

Patient info:

  1. Avoid alcohol and caffeine
  2. Take with food along with a full glass of water

Other:
Different types of emetics -> DO TO THE DOCUMENT

27
Q

Loop diuretics

Mechanism of action (3)

Indications (5)

Side effects (4)

PK/PD (2)

Patient info (2)

Renal

A

-> Furosemide, Bumetanide, Torasemide

Mechanism of action:

  1. Na+/Cl-/K+ symptom treatment antagonists
  2. Act on thick ascending loop of Henle
  3. Increase secretion of Na+, K-, Cl- and water

Indications:

  1. Hypertension
  2. Hyperkalaemia
  3. HF
  4. Cirrhosis
  5. Nephrotic syndrome

Side effects:

  1. Hypokalaemia, hypovolaemia, hyperuricaemia (increased urate reabsorption)
  2. Metabolic acidosis
  3. Abdominal pain
  4. Ototoxicity

PK/PD:

  1. 60% absorbed in patients with normal renal function
  2. Renal and hepatic excretion- increased half life for patients with renal or hepatic disease

Patient info:

  1. Avoid excess alcohol
  2. Urinary frequency increases
28
Q

Sulphonylureas

Mechanism of action

Indications

Side effects

PK/PD

Patient info

Endocrine

A

-> Gliclazide, Glimepiride

Mechanism of action:

  1. Stimulates B cells of the pancreas to produce more insulin
  2. Increase cellular glucose uptake and glycogenesis, reduces gluconeogenesis
  3. Glicazide is short acting (~12 hours)

Indications:
1. Type 2 diabetes mellitus along with diet and exercise

Side effects:

  1. Hypoglycaemia
  2. Rashes
  3. Nausea
  4. Vomiting
  5. Stomach pain
  6. Indigestion
  7. Weight gain

PK/PD:

  1. Renally excreted so accumulate in renal failure
  2. Glimepiride is long acting sulphonylureas

Patient info:

  1. Compliance important
  2. Maintain consistent diet
  3. Avoid alcohol
29
Q

GLP-1 (Glucagon like peptide) agonist

Mechanism of action (3)

Indications (1)

Side effects (4)

PK/PD (2)

Patient info (2)

Endocrine

A

-> Exanatide, Liraglutide

Mechanism of action:

  1. GLP-1 is a hormone that is released after meals to increase insulin secretion
  2. These drugs is a GLP-1 agonist
  3. It increases insulin secretion, decreases glucagon secretion and reduces hunger

Indications:
1. Type 2 Diabetes Mellitus (in association with excess weight)

Side effects:

  1. Hypoglycaemia
  2. Nausea
  3. Vomiting
  4. Diarrhoea

PK/PD:

  1. It can lower glucose alone, but when given in combination with metformin, sulfonylureas, and/or insulin it can improve glucose control
  2. Renally excreted so dose adjustment needed in renal failure

Patient info:

  1. Only given as injection
  2. Twice a day
30
Q

Anti-Thyroid drugs- Thionamides

Mechanism of action (3)

Indications (3)

Side effects (3)

PK/PD (3)

Patient info (2)

Endocrine

A

-> Carbimazole, Propylthiouracil

Mechanism of action:

  1. Reduces activity of peroxidase enzyme (required for the production of thyroid hormones)
  2. May also reduce peripheral conversion of T4 to T3
  3. Carbimazole is a pro-drug

Indications:

  1. Hyperthyroidism
  2. Thyrotoxicosis
  3. Preparing patients for thyroid surgery

Side effects:

  1. Rash
  2. Agranulocytosis
  3. Sore throat

PK/PD:

  1. Carbimazole is rapidly metabolized to thiamazole. The mean peak plasma concentration occurs at one hour
  2. It crosses the placenta and can be found in breast milk
  3. The effect of anti-thyroid drugs can take several weeks to occur so are usually prescribed alongside a beta-blocker to reduce symptoms of hyperthyroidism

Patient info:

  1. Compliance important
  2. Regular blood checks will be needed to monitor treatment response and renal, hepatic function and full blood counts
31
Q

Oral Contraceptive Pill

Mechanism of action (4)

Indications (3)

Side effects (5)

PK/PD (1)

Patient info (3)

Endocrine

A

-> Microgynon (combined oral contraceptive pill); Cerazette (progestogen only pill)

Mechanism of action:

  1. A progestin (synthetic form of progesterone) along with an oestrogen (combined oral contraceptive pill) or a progestin alone (progesterone only pill)
  2. Acts on female reproductive tract, the mammary glands, hypothalamus and the pituitary gland
  3. Reduces the production for gonadotropin releasing hormone (GnRH)
  4. Blunts the LH surge that stimulates ovulation

Indications:

  1. Contraception
  2. Menopausal and post menopausal disorders
  3. Polycystic ovarian syndrome

Side effects:

  1. Mood swings
  2. Headache
  3. Breast tenderness
  4. Increased risk of breast and ovarian cancer (small)
  5. Increased risk of venous thromboembolic in disease (small)

PK/PD:
1. Antibiotics and some enzyme inducers can reduce efficacy

Patient info:

  1. Take at the same time everyday- compliance is critical for efficacy
  2. Take with food
  3. Use alternative forms of contraception when taking concurrent antibiotics or enzyme inducers
32
Q

Opiates/ Opioids

Mechanism of action (1)

Indications (3)

Side effects ()

PK/PD ()

Patients info ()

Other ()

A

->Morphine

Mechanism of action:
1. Opioid receptor agonist, acts on mu, kappa and delta on presynaptic neurons. this gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system

Indications:

  1. Acute severe pain (including in setting of myocardial infarction)
  2. Acute pulmonary oedema
  3. Chronic pain

Side effects:

  1. Nausea
  2. Vomiting
  3. Abdominal pain
  4. Constipation
  5. Respiratory depression
  6. Sedation

PK/PD:

  1. Predominantly metabolized by the liver
  2. Opioid receptor agonist, acts on mu, kappa and delta on presynaptic neuroses. This gives numerous effects that increase nociceptive thresholds throughout the central and peripheral nervous system
  3. Metabolized are active and can accumulate in renal failure
  4. Accumulation can result in respiratory and central nervous system depression

Patient info:
1. Often given with an anti-emetic to reduce nausea/vomiting

33
Q

Non-selective NSAIDs

Mechanism of action (2)

Indications (3)

Side effects (7)

PK/PD (3)

Patients info (4)

A

-> Ibuprofen, Diclofenac

Mechanism of action:

  1. Non-selective inhibition of cyclo-oxygenate (COX1 and 2) enzymes, decreasing key inflammatory mediator prostaglandin from being synthesised
  2. Reduces pain, inflammation and swelling

Indications:

  1. Mild to moderate pain relief
  2. Rheumatic disorders (such as RA and osteoarthritis)
  3. Fever (anti-pyretic effect)

Side effects:

  1. Gastric and duodenal ulceration (risk increases with duration of therapy and dosage)
  2. Nausea
  3. Diarrhoea
  4. Small increased risk of thrombotic events even when used short term, particularly diclofenac and high dose ibuprofen
  5. Avoid in pregnancy particularly 3rd trimester (risk of closure of fetal ductus arteries us in uterus and pulmonary hypertension in newborn)
  6. Renal impairment
  7. Hyperkalaemia

PK/PD:

  1. Pain relief starts soon after the first dose, full analgesic effects can take up to one week and anti-inflammatory effects can take up to 3 weeks
  2. Avoid in patients with renal impoairment- use lowest dose, for shortest time if unavoidable.
  3. Caution should be used in the elderly- risk of GI bleeds.

Patient info:

  1. Risk of stomach bleeds if on long-term use
  2. Take with food or milk, to reduce abdominal discomfort and to reduce the risk of bleeding
  3. Take only when required
  4. In elderly patients a proton pump inhibitor is usually given alongside NSAID drugs
34
Q

Paracetamol

Mechanism of action (2)

Indications (2)

Side effects (1)

PK/PD ()

Patient info ()

Other ()

A

-> Paracetamol

Mechanism of action:

  1. A weak cyclooxygenase enzyme (COX) inhibitor with selectivity for brain COX
  2. Lacks peripheral anti-inflammatory actions but is useful in increasing the threshold for nociceptive activation by inhibiting prostaglandin synthesis and its effects centrally

Indications:

  1. Mild to moderate pain relief
  2. Fever (anti-pyretic effect)

Side effects:
1. Rash/ blood disorders (rare)

PK/PD:

  1. Overdose must be avoided- severe liver damage can occur and can be fatal
  2. Careful dosing in younger patients and patients with low body weight (reduce dose to 500mg 4-6 hourly, aid in patients <50kg)

Patient info:
1. Take only the prescribed amount and be wary of other over-the-counter medications that may contain paracetamol

MBChB Phase 3 (2 decks)

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