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MBChB Phase 3 > Phase 3 Pharmacology - 50 Drugs List > Flashcards

Phase 3 Pharmacology - 50 Drugs List Flashcards

1
Q

Acetylsalicylic Acid

MoA (4)
Indication (2)
Side effects (5)
PK and PD (1)
PI (2)
A

AKA Aspirin!

Mechanism of Action of 4 simple steps. Nice!

  1. Irreversible inactivation of COX enzyme
  2. Reduction of Thromboxane and Prostaglandins
  3. Reduced platelet activity, reduced thrombus formation “blood thinner”
  4. Reduced prostaglandin synthesis decreases nociceptive sensitization and inflammation “pain killer”

Indications. Two!

  1. Secondary prevention thrombotic events
  2. Pain relief

Side effects. Five!

  1. Bleeding
  2. Peptic Ulceration
  3. Angioedema
  4. Bronchospasm
  5. Reye’s Syndrome (rare!) - associated with viral infection in children. Encephalopathy and liver damage.

PD/PK
Half life increases with increasing doses due to non-linear pharmacokinetics.

Patient Information:
Avoid OTC preps containing Aspirin
Long term Aspirin use indicated PPIs.

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2
Q

Recombinant Tissue Plasminogen Activator (rtPA)

MoA (3)
Indication (3)
Side effects (2)
PK and PD (3)
PI (1)
A

Tenecteplase
Alteplase

MoA (3)

  1. Recombinant form of Tissue Plasminogen Activator
  2. Catalyses conversion of plasminogen to plasmin.
  3. Promotes fibrin clot lysis

Indication(s) (3)

  1. Acute Ischaemic Stroke within 4.5 hours of onset
  2. Myocardial Infarction within 12 hours on onset
  3. Massive pulmonary embolism

*Not all thrombolytics are licensed for this use.

Side Effects (2)

  1. Bleeding
  2. Allergic Reaction/ Angio-oedema

PKPD (3)

  1. Altephase: Bolus-infusion regimen
  2. Tenectplase: Single Bolus
  3. Will interact with other haematological agents.

PI (1)
1. Risk:benefit, consider risk of bleeding complications.

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3
Q

Low Molecular Weight Heparin

MoA (4)
Indication (3)
Side effects (3)
PK and PD (6)
PI (3)
A

Low Molecular Weight Heparin

MoA

  1. Enhances activity of antithrombin III
  2. Antithrombin III, inhibits thrombin
  3. Heparins also inhibit multiple other factors
  4. Over all anticoagulant effect.

Indications

  1. Treatment and prophylaxis of thromoembolic diseases, including induction of vitamin K antagonist
  2. Renal Dialysis
  3. Acute Coronary Syndrome

Side effects

  1. Bleeding (Major Haemorrhage risk 3.5%)
  2. Heparin induced thrombocytopenia (but less than unfractioned heparin)
  3. Osteoporosis (but less than unfractioned heparin)

PK/PD

  1. Subcut injection
  2. More predictable dose-response than unfractioned heparin.
  3. 2-4 times longers plasma half-life than unfractioned heparin
  4. Clearance mostly via renal pathway, so consider this in patients with renal failure.
  5. Regular coagulation monitoring not required
  6. Less readily reversable with protamine than unfractioned heparin

PI

  1. Risk of bleeding
  2. Requires an injection
  3. Will need monitoring over long use (FBC)
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4
Q

Factor Xa Antagonists

MoA (2)

Indication (2)

Side effects (2)

PK and PD (4)

PI (1)

A

A P I X A B A N

MoA:

  1. Inhibits the conversion of prothrombin to thrombin
  2. Prevents formation of fibrin clots

Indication(s):

  1. Prophylaxis of venous thromboemolism following knee or hip surgery
  2. Thromboprophylaxis in non-valvular AF

Side effects:

  1. Bleeding
  2. Nausea

PK/PD

  1. Predictable drug interactions
  2. 75% is metabolised by the liver, the rest is renally excreted
  3. No need for therapeutic monitoring
  4. No antidote

PI
1. Bleeding

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5
Q

Direct Thrombin Inhibitor

MoA (2)

Indication (2)

Side effects (2)

PK and PD (4)

PI (1)

A

D A B I G A T R A N

MoA:

  1. Direct thrombin inhibitor, prevents the conversion of fibrinogen to fibrin.
  2. No thrombus. anticoagulation

Indications:

  1. Prophylaxis of thromboemolism. Ideal for post op!)
  2. Thromboprophylaxis in non-valvular AF

Side Effect:

  1. Bleeding
  2. Dyspepsia

PK/PD

  1. Rapid onset of action
  2. No food and few drug interactions (does not metabolise via CYP 450)

PI
Risk of bleeding

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6
Q

Non-cardioselective Beta Blockers

MoA (3)

Indication (6)

Side effects (7)

PK and PD (4)

PI (3)

A

P R O P A N O L O L
C A R V E D I L O L

MoA:
Propranolol: B1 Adrenoreceptor Antagonist
Carvedilol: B1, B2, A1 Adrenergic Receptor “Antagonist effects”
Overall inhibits stimulation of heart and vascular smooth muscle.

Indications:
Hypertension
Angina
Anxiety
Migraine Prophylaxis
Post-MI Prophylaxis
Carvedilol or Bisoprolol can be used as supportive treatment in HF.
Side Effects:
Hypotension
Bradycardia
Bronchospasms
Fatigue
Cold Extremities
Sleep Disturbance
Loss of hypoglycemic awareness

PK/PD

  1. Be wary in diabetic patients - deranged carb metabolism.
  2. Avoid in Asthma/ COPD patients due to bronchospasm.
  3. Do not combine with rate limiting calcium channel blockers in anti-hypertensive treatment
  4. Pronanolol is lipid soluble and is mainly cleared by the liver. Avoid in liver impairment, and avoid abrupt withdrawal.

PI
Nightmares
Compliance is key, hypertension can be asymptomatic.
Fatigue and cold extremities common.

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7
Q

Nitrates
(Such as Glyceryl Trinitrate)

MoA (3)

Indication (2)

Side effects (3)

PK and PD (3)

PI (3)

A

GLYCERYL TRINITRATE
ISOSORBIDE MONONITRATE

MoA:

  1. Converted to Nitric Oxide (NO). Strong vasodilator.
  2. Cardioselective acts mostly on coronary blood vessels.
  3. Reduces myocardial oxygen consumption via reducing cardiac preload/ afterload.

Indications:

  1. Angina
  2. Severe Hypertension

Side Effects:

  1. Headache
  2. Postural Hypotension
  3. Tachycardia

PK/PD

  1. Tolerance over time
  2. Isosorbide mononitrate has a longer duration of action.
  3. GTN is rapidly deactivated by hepatic metabolism hence spray/ sublingual tablet/ IV.

PI

  1. Avoid tolerance by having a daily nitrate free period.
  2. Headaches usually subside
  3. Take GTN prior to activity
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8
Q

Non rate-limiting calcium channel blockers

MoA (4)

Indication (2)

Side effects (4)

PK and PD (3)

PI (3)

A

AMLODIPINE
NIFEDIPINE
FELODIPINE

“DIPINE”

MoA:

  1. Blocks L-Type Calcium Channel Blockers
  2. Smooth muscle depression
  3. Coronary blood vessels dilatation and reduced afterload

Indications:

  1. Stable Angina
  2. Hypertension

Side Effects:

  1. Ankle oedema
  2. Abdominal pain
  3. Nausea
  4. Palpitations (this drug rarely lowers HR, rather can increase it)
  5. Flushing/ headache/ dizziness

PK/PD

  1. Avoid in cardiogenic shock
  2. Avoid in unstable angina
  3. Avoid in Significant Aortic Stenosis

PI:

  1. COMPLY
  2. Hypertension is asymptomatic, it still needs to be controlled
  3. Hot weather will worsen oedema.
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9
Q

Cardiac Glycosides

MoA (4)

Indication (2)

Side effects (4)

PK and PD (6)

PI (1)

A

DIGOXIN

MoA:

  1. Increases vagal parasympathetic activity and inhibits the NA/K Pump.
  2. Causes a build up of Na in the cell.
  3. More Ca is brought into the cell via Na/Ca exchangers
  4. Build up of Ca increases force of contraction and reduces rate of conduction through AV node.

Indication:

  1. Heart Failure
  2. HR control in AF

Side effects:

  1. Nausea
  2. Vomiting
  3. Diarrhoea
  4. Confusion
  5. Arrhythmia

PK/PD

  1. Narrow Therapeutic Index
  2. Symptoms of toxicity similar to clinical deterioration (?)
  3. Plasma concentration is a poor indicator of toxicity
  4. Antibody fragments (specific to Digoxin) can be used to treat overdose
  5. Long half life.
  6. Renal function, age and heart disease status is key.

PI:
1. Be aware of Digitalis Toxicity

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10
Q

Penicillins (Beta Lactams)

MoA (3)

Indication (2)

Side effects (4)

PK and PD (3)

PI (3)

A

PENICILLIN V
FLUCLOXACILLIN
BENZYLPENICILLIN
AMOXICILLIN

MoA:

  1. Attaches to penicillin-binding-proteins on bacterial cell walls being formed.
  2. Inhibits transpeptidase enzyme
  3. Cell wall fails to cross link, cell autolyses

Indications:
Specific to bacterial infection. Provides a broad spectrum of cover.

Examples:

  1. Flucloxacillin for Otitis Externa
  2. Amoxicillin for non-severe community acquired pneumonia

Side effects:

  1. Diarrhoea
  2. Vomiting
  3. Liver function impairment
  4. Hypersensitivity reactions

PK/PD

  1. Orally taken
  2. Flucloxacillin is resistant to Beta-Lactamases
  3. Amoxicillin is susceptible to Beta-Lactamases (Can be given with a Beta-Lactamase Inhibitor, Clavulonic Acid.

PI:

  1. Bacterial resistance is possible (End of the world)
  2. Diarrhoea is common
  3. Rash? Report! It’s a sign of hypersensitivity. NO PEN.
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11
Q

Glycopeptides

MoA (1)

Indication (3)

Side effects (7)

PK and PD (3)

PI (3)

A

VANCOMYCIN

MoA:
1. Bactericidal against gram +ve bacteria. Inhibits cell wall synthesis.

Indications:

  1. Severe Gram +ve infection
  2. MRSA
  3. Severe C.diff infection

Side Effects:

  1. Fever
  2. Rash
  3. Local phlebitis at injection site
  4. Nephrotoxicity (age related risk)
  5. Ototoxicity (rare)
  6. Blood disorders such as neutropenia
  7. Anaphylactoid reaction “redman” if infusion is too fast.

PK/PD

  1. Infusion continuous or pulsed.
  2. Long duration, 12 hours between doses is okay.
  3. Narrow therapeutic range

PI:

  1. Risk of kidney damage
  2. Report changes in hearing
  3. Regular bloods are needed
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12
Q

Quinolones

MoA (1)

Indication (6)

Side effects (4)

PK and PD (-)

PI (1)

A

CIPROFLOXACIN

MoA:
1. Mashes up DNA repair and replication.

Indications:

  1. Gram -ve / +ve infections “Broad Spectrum”
  2. Respiratory tract infection
  3. Upper urinary tract infection
  4. Peritoneal infection
  5. Gonorrhoea
  6. Prostatitis

Side Effects:

  1. GI toxicity
  2. QT wave prolongation
  3. C.Diff infection (antibiotic associated)
  4. Tendonitis (rare)

PK/PD
None listed

PI:
1. Risk of diarrhoea

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13
Q

Inhibitors of Folate Synthesis

MoA (1)

Indication (4)

Side effects (7)

PK and PD (3)

PI (3)

A

TRIMETHOPRIM

MoA:
1. Inhibits the folate metabolism pathway, impairs DNA synthesis.

Indication:

  1. First line antibiotic in uncomplicated UTI
  2. Acute/ chronic bronchitis
  3. Pneumocystis pneumonias (PCP)
  4. Broad spectrum, provides MRSA cover

Side effects:

  1. Elevated serum creatinine
  2. Hyperkalaemia
  3. Depressed haematopoeisis
  4. Rash and GI disturbance (common-ish).

PK/PD

  1. Bloods to monitor
  2. Resistance can occur
  3. Rash and GI disturbances common
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14
Q

Beta-Adrenergic Bronchodilators

MoA (5)

Indication (2)

Side effects (4)

PK and PD (1)

PI (3)

A

SALBUTAMOL

MoA:

  1. Short acting beta-2 adrenoreceptor agonist (SABA).
  2. Relaxes bronchial smooth muscle (hence bronchodilation).
  3. Inhibit pro-inflammatory cytokine release from mast cells
  4. Inhibits TNA-a release from monocytes
  5. Increases cilia action: mucus clearance

Indications:

  1. Asthma
  2. COPD

Side Effects:

  1. Tremor
  2. Tachycardia
  3. Headace
  4. Sleep disturbances

PK/PD
1. Small amount of inhaled drug will reach the lungs, hence the use of a spacer.

PI:

  1. Strict compliance to technique
  2. Take before exercise
  3. If needed more than once daily: revew.
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15
Q

Anti-Muscarinic Bronchodilators

MoA (2)

Indication (3)

Side effects (3)

PK and PD (2)

PI (2)

A

TIOTROPIUM
IPRATROPPRIUM BROMIDE

MoA:

  1. Muscarinic Receptor (M3) antagonist, produces bronchodilatory effects.
  2. Reduces mucus secretion

Indications

  1. Asthma
  2. COPD
  3. Rhinitis

Side effects:

  1. Dry mouth
  2. Cough
  3. Constipation

PK/PD

  1. Inhaled and poorly absorbed into circulation
  2. Nebulised IB through mouthpiece to reduce risk of Acute Angle Closure Glaucoma

PI

  1. Technique
  2. May cause a cough
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16
Q

Anti-Histamines (H1 receptor antagonists)

MoA (2)

Indication (4)

Side effects (2)

PK and PD (2)

PI (2)

A 
CHLOROPHENIRAMINE
DESLORATIDINE
FEXOFENADINE
HYDROXYZINE
CETIRIZINE HYDROCHLORIDE

MoA:

  1. Antihistamine H1 Receptor Agonist
  2. Inhibits histamine-mediated contraction and vasodilation of the bronchial smooth muscle

Indications:

  1. Anaphylaxis
  2. Hay Fever
  3. Urticaria
  4. Sedation

Side Effects:

  1. Drowsiness
  2. Tinnitus

PK/PD

  1. Renal excretion
  2. Sedation arises from CNS H1 Antagonism. (Second generation H1RAs do not cross BBB so do not cause drowsiness in therapeutic doses)

PI:

  1. Do not operate heavy machinery if you feel side effects
  2. Do not drive if you feel side effects
17
Q

Dopamine Agonists

MoA (3)

Indication (1)

Side effects (2)

PK and PD (3)

PI (2)

A 
APOMORPHINE
PRAMIPEXOLE
BROMOCRIPTINE
PERGOGLIDE
ROTIGOTINE

MoA:

  1. Stimulate post synaptic dopamine receptors
  2. Apomorphine works in a non selective manner on D1/D2Rs
  3. Pramipexole works selectively against D3Rs.

Indications:
1. Parkinsons

Side Effects:

  1. Apomorphine (3): pain at site of injection, nausea, vomiting.
  2. Praxopexole (4): hallucinations, nausea, drowsiness, involuntary movements

PK/PD:

  1. Apomorphine: highly emetic so limited use, short half life of 40mins. Injection.
  2. Pramipexole: Cimetidine increases toxicity, long half life of 8hrs.
  3. Dopamine agonists reduce in efficacy over time

PI:

  1. Apomorphine is injected
  2. Dopamine agonists are weaker than L-DOPA so treatment may be modified in time.
18
Q

Anti Epileptic Drugs (CARBAMAZEPINE)

MoA (2)

Indication (3)

Side effects (9)

PK and PD (6)

PI (2)

A

CARBAMAZEPINE

MoA:

  1. Antagonist of Voltage Gated Na channels on pre-synaptic membrane
  2. Reduced neuronal excitability and action potential.

Indications:

  1. Epilepsy
  2. Trigeminal Neuralgia
  3. Neuropathic Pain

Side Effects:

  1. Dizziness
  2. Dry Mouth
  3. Ataxia (Lack of voluntary muscle movement)
  4. Fatigue
  5. Headache
  6. Diploplia (double vision)
  7. Blurred Vision
  8. Hyponatraemia
  9. Stevens-Johnson Syndrome (rare)

PK/PD

  1. Response to the drug can vary
  2. Induces metabolism of itself via CYP450
  3. Interacts with other anti-convulsants
  4. Prone to resistance by RALBP1
  5. Avoid grapefruit. It can raise serum levels of this drug.
  6. HLA-B*1502 allele raises risk of Stevens-Johnson Syndrome.

PI:

  1. Avoid alcohol
  2. Avoid grapefruit

Summary of Mechanism of Action of Anti-Epileptic Drugs

  1. Reduce pre-synaptic excitability
    a. Voltage-gated Na+ channel antagonist (carbamazepine, lamotrigrine)

b. Voltage-gated K+ channel agonist (retigabine)
2. Stops neurotransmitter release
a. SV2A vesicle antagonist (levetiracetam)
b. Voltage-gated Ca2+ channel antagonist (pregablin and gabapentin)

  1. GABA-ergic system agonists
    a. GABA metabolism inhibitor (valproate, vigabatrin)

b. GABA transporter antagonist (tiagabine)

  1. Reduces post-synaptic excitability
    a. GABA receptor agonist (benzodiazepines)

b. AMPA and NMDA receptor antagonist

19
Q

Anti Epileptic Drugs (PHENYTOIN)

MoA (2)

Indication (2)

Side effects (10)

PK and PD (6)

PI (2)

A

PHENYTOIN

MoA:

  1. Antagonist of Voltage Gated Na channels on pre-synaptic membrane
  2. Reduced neuronal excitability and action potential.

Indications:

  1. Epilepsy
  2. Trigeminal Neuralgia

Side Effects:

  1. Insomnia
  2. Headache
  3. Rash
  4. Constipation
  5. Vomiting
  6. Gingival hyperplasia (growth of gums)
  7. Liver damage
  8. Stevens-Johnson Syndrome (rare)
  9. Leucopenia (rare)
  10. Thrombocytopenia (rare)

PK/PD

  1. Narrow therapeutic index
  2. Induces metabolism of itself via CYP450
  3. Interacts with other anti-epileptics
  4. Non-linear drug/dose relationship

PI:

  1. Avoid Alcohol
  2. Avoid calcium, aluminum, magnesium and iron supplements for 2 hours post dose.
  3. Take with food
20
Q

Anti-Epileptic Drugs (LEVETIRACETAM)

MoA (3)

Indication (1)

Side effects (6)

PK and PD (3)

PI (2)

A

LEVETIRACETAM

MoA:

  1. SC2A is a synaptic vesicle protein required for neurotransmitter release
  2. Levetiracetam blocks this and reduces neurotransmitter release
  3. This induces an anti-epileptic effect

Side effects:

  1. Headache
  2. Fatigue
  3. Anxiety
  4. Irritability
  5. Drowsiness
  6. Constipation

PK/PD

  1. Rapid absorption after oral administration
  2. Food does not affect bioavailability
  3. Cytochrome P450 is not involved in it’s metabolism

PI:

  1. Do not operate heavy machinery if you feel side effects
  2. Not recommended in pregnancy or during breastfeeding
21
Q

Tricyclic Antidepressants

MoA (3)

Indication (3)

Side effects (3)

PK and PD (3)

PI (1)

A

AMITRIPTYLINE
IMIPRAMINE
DOXEPIN

MoA:

  1. Stops reuptake of monoamines
  2. Binds monoamine pump at pre-synaptic cleft
  3. Reduced reuptake of NA and/or Serotonin combats symptoms of depression

Indications:

  1. Depression
  2. Panic Disorders
  3. Neuropathic Pain

Side Effects:

  1. Sedation
  2. Postural hypertension and tachycardia (due to anti-adrenergic effects)
  3. Urinary retention, dry mouth, blurred vision (due to anti-cholinergic effects)

PK/PD

  1. Blocks histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects
  2. Well absorbed orally
  3. First pass effect (liver)

PI:
1. Suppression of symptoms may take weeks to appear

22
Q

Benzodiazepines

MoA (3)

Indication (4)

Side effects (4)

PK and PD (3)

PI (1)

A

DIAZEPAM
LARAZEPAM
MIDAZOLAM

MoA:

  1. Increases GABA-R affinity to GABA
  2. GABA binding causes increased chloride flow through chloride channels
  3. Hyperpolatization occurs: reducing activity of limbic, thalamic and hypothalamic regions of the brain

Indications:

  1. Anxiety
  2. Epilepsy
  3. Muscle Spasm
  4. Alcohol Withdrawal

Side effects

  1. Sedation
  2. Ataxia
  3. Altered Mental Status
  4. Insomnia

PK/PD

  1. Diazepam will accumulate in long term use in patients with liver failure. Mucosal absorption.
  2. Lorazepam accumulates to a lesser degree so is preferred for patients with liver failure. Will not work via rectal route.
  3. Midazolam is potent and short acting, parental preferred.

PI:

  1. Report SOB or palpitations
  2. Only for short term, risk of addiction
23
Q

Anti-TNF agents

MoA (4)

Indication (4)

Side effects (3)

PK and PD (3)

PI (1)

A

ETANERCEPT
INFLIXIMAV (MOAB)
ADILMUMAB (MOAB)

MoA

  1. Anti TNF-A/B
  2. Blocks binding to Receptors
  3. Secretion of IL1, 6, 8 inhibited from M.Os and T Cells
  4. Reduced inflammation

Indications

  1. Rheumatoid Arthritis
  2. Psoriatic Arthritis
  3. Ankylosing Spondyltis
  4. Juvenile Arthritis

Side Effects:

  1. Injection site reactions
  2. Flu like symptoms
  3. Immune deficiency

PK/PD
1. Parental route. Subcut injection.

PI:
1. Maintain good hygiene and report symptoms of infection.

24
Q

Proton Pump Inhibitors

MoA (2)

Indication (5)

Side effects (5)

PK and PD (1)

PI (2)

A

OMEPRAZOLE
LANSOPRAZOLE
PANTOPRAZOLE

MoA:

  1. Binds H+/K+ATPase in Gastric Parietal Cells
  2. Reduces HCL production, thus reduced gastric activity

Indications:

  1. Peptic Ulcers
  2. GORD
  3. H.pylori Infection
  4. Prophylaxis in patients on long term NSAIDS
  5. Zollinger-Ellison Syndrome

Side Effects:

  1. Nausea
  2. Vomiting
  3. Insomnia
  4. Vertigo
  5. Headaches

PK/PD

  1. Avoid alcohol
  2. Take before food (30/60 minutes)
25
Q

Laxatives

MoA (2)

Indication (3)

Side effects (4)

PK and PD (2)

PI (1)

A

LACTULOSE
SENNA

MoA:

  1. Lactulose: Reduces water reabsorption in the intestine, pulling water into the bowel hence increased motility.
  2. Senna: stimulates/ irritates the intestine.

Indications

  1. Constipation
  2. Pregnancy
  3. Prophylaxis in opiate analgaesia

Side effects:

  1. Dehydration
  2. Salt loss
  3. Abdominal Cramps
  4. Fatigue

PK/PD

  1. Lactulose: Consists of fructose and galactose. Breakdown by colonic bacteria increases the osmotic pressure
  2. Short term only, risk of organ failure in prolonged use.

PI:
1. Take liberally without regard to meals.

26
Q

Anti Emetics

MoA (4)

Indication (3)

Side effects (5)

PK and PD (2)

PI (2)

A

METOCLOPRAMIDE

MoA:

  1. Dopamine Receptor (D2) Antagonist
  2. Raises activity in the chemoreceptor trigger zone - reduces input from afferent visceral nerves
  3. Also increases gastric emptying and intestinal transit
  4. Reduced oesophageal reflux

Indications:

  1. Nausea
  2. Vomiting
  3. To increase gastric emptying

Side effects:

  1. Dystonia
  2. Confusion
  3. Dizziness
  4. Diarrhoea
  5. Parkinsonism in long term use

PK/PD:

  1. Oral or parental route
  2. Dystonic reactions risk increase at extremes of age

PI:

  1. Avoid Alcohol
  2. Take 30 minutes before meal
27
Q

Thiazide Diuretics

MoA (2)

Indication (2)

Side effects (7)

PK and PD (2)

PI (3)

A

BENDROFLUMETHIAZIDE
INDAPAMIDE
CHLORTALIDONE

MoA:

  1. Inhibits NA+/CL- transporter at DCT and CD.
  2. Increases these ions excretion (and with it, water)

Indications:

  1. Hypertension
  2. Oedema of cardiac/ renal/ hepatic or iatrogenic origin

Side Effects:

  1. Hypokalaemia
  2. Hypomagnesaemia
  3. Hyponatraemia
  4. Hypercalcaemia
  5. Hyperuricaemia
  6. Reduced glucose tolerance
  7. Hypersensitivity reactions (rashes, pneumonitis) - rare.

PK/PD

  1. Produces diuresis quickly, within 1-2 hours.
  2. Reduced efficacy with NSAID use.

PI:

  1. Urinary frequency usually not affected
  2. Report a sudden rash
  3. Risk of electrolyte imbalance
28
Q

Insulin

MoA (3)

Indication (3)

Side effects (4)

PK and PD (2)

PI (3)

A

NOVORAPID
ACTRAPID
GLARGINE
HUMALOG MIX

MoA:

  1. Insulin increases cellular uptake of Glucose.
  2. Simulates glycogenesis, encourages DNA synthesis and promotes release of growth hormone
  3. Novorapid, Actrapid, Glargine and Humalog Mix are short, short, long, intermediate acting respectively.

Indications:

  1. T1DM
  2. T2DM
  3. Hyperkalaemia

Side effects:

  1. Hypoglycaemia
  2. Symptoms of Hypo
  3. Oedema
  4. Injection site reactions

PK/PD

  1. Type and dose depend on lifestyle
  2. Subcut. ACTRAPID can be IV.

PI:

  1. Injected
  2. Compliance
  3. Do not skip meals on insulin
29
Q

Biguanides

MoA (3)

Indication (2)

Side effects (6)

PK and PD (2)

PI (2)

A

METFORMIN

MoA:

  1. Increases activity of AMPK
  2. Inhibits gluconeogenesis
  3. Reduces insulin resistance

Indications:

  1. T2DM
  2. POS

Side effects:

  1. Diarrhoea
  2. Nausea
  3. Vomiting
  4. Taste disturbance
  5. Lack of appetite
  6. Risk of lactic acidosis in renal failure

PK/PD

  1. Not recommended in pregnancy or renal failure (eGFR <30mls/min)
  2. Absorption reduces when taken with food

PI:

  1. Take at same time everyday
  2. Avoid alcohol
30
Q

Synthetic Thyroid Hormone

MoA (4)

Indication (2)

Side effects (6)

PK and PD (3)

PI (1)

A

LEVOTHYROXINE

MoA:

  1. Thyroxine increases basal metabolic rate
  2. Levothyroxine replaces Thyroxine in deficiency
  3. Acts like T4, converted to T3.
  4. Maintains brain function, food metabolism, body temp etc.

Indications:

  1. Hypothyroidism
  2. Chronic Lymphocytic Thyroiditis

Side effects:

  1. Chest Pain
  2. Coma
  3. Diarrhoea
  4. Tachycardia
  5. Itching
  6. Muscle Cramps

*if dosing correct, side effects unusual

PK/PD

  1. Primarily renal excretion
  2. IV
  3. Half life of 6-7 days. Review at 6 weeks.

PI:
1. Take 30-60 minutes before breakfast

31
Q

Bisphosphates

MoA (2)

Indication (3)

Side effects (5)

PK and PD (1)

PI (2)

A

ALENDRONATE
IBANDRONATE

MoA:

  1. Inhibits osteoclast bone resorption
  2. No effect on bone formation

Indications:

  1. Post menopausal osteoporosis
  2. Reduction of risk in vertebral and hip #
  3. Paget’s Disease

Side effects:

  1. Abdominal pain
  2. Dyspepsia
  3. Acid regurge
  4. Dysphagia
  5. Headache

PK/PD
1. Bioavailability reduced at breakfast with ingestion of coffee/ orange juice

PI:

  1. Take 30 minutes before breakfast
  2. Avoid caffeine
32
Q

Opiates / Opioids (CODEINE)

MoA (1)

Indication (3)

Side effects (5)

PK and PD (4)

PI (2)

A

CODEINE

MoA:
1. Opioid Receptor Agonist: acts pre-synaptic neurones (mu, kappa, delta). Increases nociceptive thresholds in the CNS/ PNS.

Indications:

  1. Mild/ moderate pain
  2. Persistent dry cough
  3. Diarrhoea

Side effects:

  1. Nausea
  2. Vomiting
  3. Constipation
  4. Biliary Spasm
  5. Headache on withdrawal

PK/PD

  1. Metabolised to Morphine
  2. Mainly metabolised by liver
  3. Renal excretion. Accumulates in renal failure.
  4. 10% population resistant, lack demethylating enzyme so Morphine is not produced

PI:

  1. Can be taken with paracetamol
  2. Constipation a likely side effect
33
Q

Opiates / Opioids (OXYCODONE)

MoA (1)

Indication (3)

Side effects (4)

PK and PD (3)

PI (1)

A

OXYCODONE

MoA:
1. Opioid Receptor Agonist: acts pre-synaptic neurones (mu, kappa, delta). Increases nociceptive thresholds in the CNS/ PNS.

Indications:

  1. Moderate to severe pain in cancer patients
  2. Postop pain
  3. Severe pain

Side effects:

  1. Nausea
  2. Vomiting
  3. Abdominal Pain
  4. Constipation

PK/PD:

  1. Long and short acting preparations
  2. Metabolised by liver
  3. IV/ Subcut. Slow infusion.

PI:
1. Nausea and constipation common

34
Q

Selective NSAIDS

MoA (2)

Indication (1)

Side effects (5)

PK and PD (5)

PI (3)

A

CELECOXIB

MoA:

  1. Selective inhibitor of COX-2 (reduces Prostaglandin)
  2. Reduces pain and swelling

Indications:
1. Pain and inflammation in osteoarthritis, rheumatoid arthritis and ankylosing spondylitis

Side Effects:

  1. GI Ulcers
  2. Nausea
  3. Diarrhoea
  4. Renal impairment
  5. Hyperkalaemia

PK/PD

  1. GI ulcer incidents lower compared to non selective NSAIDs.
  2. Higher risk of Cardiovascular events
  3. Avoid in renal impairment, or at least minimise
  4. Caution in use in elderly
  5. Avoid in pregnancy’s in 3rd trimester

PI:

  1. Risk of GI bleed
  2. Take with food or milk
  3. Take only when required
35
Q

Xanthine Oxidase Inhibitors

MoA (2)

Indication (3)

Side effects (4)

PK and PD (3)

PI (4)

A

ALLOPURINOL

MoA:

  1. Reduces synthesis of Uric Acid. Competitive inhibition.
  2. Reduces serum Uric Acid

Indications

  1. Prophylaxis of Gout
  2. Prophylaxis of calcium oxalate renal stones
  3. Hyperuricaemia in cancer chemotherapy

Side effects:

  1. Rash
  2. Hypersensitivity
  3. GI Disturbance
  4. Neutropenia (rare)

PK/PD

  1. Not used to treat acute gout and it can exacerbate acute episodes.
  2. Inhibits CYP450
  3. Affects metabolism of Azathioprine

PI:

  1. Rash and GI disturbance fairly common
  2. Report rash
  3. Compliance
  4. NSAID or Cochicine prescribed in first months of therapy to prevent exacerbation of gout.

MBChB Phase 3 (2 decks)

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