Pharmacology Flashcards
Define Affinity
the tendency of a molecule to bind to a receptor
Define Efficacy
how well an agonist achieves a response
Define an antagonist
A chemical that opposes the action of another chemical.
Therefore, antagonists should have no action on their targets in the absence of an agonist.
Drugs that can cause hyperkalaemia (10)
THANKS CYCLE PENines
T: Trimethoprim
H: Heparin (LMWH - inhibition of aldosterone synthesis)
A: ARBs and ACE-Is (reduce aldosterone -> potassium retention)
N: NSAIDs
K: K+ sparing diuretics
S: Succinyl choline
CYCLE: Cylosporins and Tacrolimus
PENines: Pentamidine
Drugs that can cause hypokalaemia (7)
DIG CBT D: Diuretics and laxatives I: Insulin G: Gentamicin C: Corticosteroids (Pred) B: Beta-2-agonists T: Theophylline
Drugs that can cause hypercalcaemia (2)
- Vit D
- Thiazide diuretics
Drugs that can cause hypocalcaemia (3)
- Bisphosphonates
- Corticosteroids
- Loop diuretics
Drugs that can cause hypernatraemia (1)
- Lithium
Drugs that can cause hyponatraemia (5)`
- Antidepressants (SSRIs, tricyclics)
- Laxatives
- Loop diuretics
- Thiazide diuretics
- Potassium-sparing diuretics
- Sulfonylureas
- Carbamazepine
- Vincristine
- Cyclophosphamide
Drugs that should be stopped before surgery? (8)
- Aspirin (unless recent ACS, coronary artery stent or ischaemic stroke) -> replace with LMWH or unfractionated heparin
- COCP
- MAOIs
- Lithium (24 hrs before major surgery only, monitor fluids and electrolytes in minor surgery)
- Potassium-sparing diuretics on morning of surgery
- ACE-Is and ARBs 24 hrs before
- Herbal medicines
- Let surgeon know if on tricyclic antidepressants
Drugs to be stopped in AKI
Direct nephrotoxics:
- ACE-Is (small creatinine rise expected when initiating, recheck in 1 week)
- ARBs
- Diuretics (Furosemide, Potassium-sparing)
- NSAIDs
- Contrast media
Stop in AKI:
- Allopurinol (can accumulate) - max of 100 mg OD until improves
- Hypoglycaemic agents - modified-release
- Gentamicin/Vancomycin
- Lithium
- Methotrexate
- Metformin (avoid if GFR <30)
- CCBs
- Tetracyclines
- Trimethoprim
- Statin (if rhabdomyolysis)
Drugs that can cause confusion
Sedatives:
- Benzos
- Opioids
- Glucocorticoids (Prednisolone)
Drugs that can cause hyperglycemia
- Glucocorticoids (Pred)
- Atypical antipsychotics (Clozapine)
- Thiazide diuretics
- Statins
Trimethoprim:
- Dose, CI, Cautions, SEs
- Interaction
- Pregnancy
- Dose: 200 mg BD for 3 days (7 days in males
- CI: Blood dyscrasias
- Cautions:
- Blocks folate metabolism, may exacerbate pre-existing folate deficiency, generally doesn’t prevent short term use (do NOT prescribe with methotrexate)
- Porphyrias
- Renal dysfunction: half dose if eGFR < 15
- SEs: Diarrhoea, vomiting, electrolyte imbalance, headache, nausea, skin reactions
- Interactions: METHOTREXATE
- Teratogenic in FIRST TRIMESTER
Nitrofurantoin:
- Dose, CI, Cautions
- Pregnancy
- Dose: 50 mg QDS for 3 days (7 days in males)
- Avoided if eGFR less than 45
- Used with caution if eGFR 30-44 (short course only: 3-7 days)
- CI: Porphyrias, G6PD deficiency, eGFR < 45
- Cautions:
- Anaemia, DM, electrolyte imbalance, folate deficiency, urine may be yellow/brown
- Teratogenic at TERM
Anticoagulation before surgery
- If AF-related stroke/TIA then need formal anticoagulation with treatment dose LMWH
- Without this Hx, no need for formal anticoag
- BNF recommends that if INR > 1.5 before elective surgery, phytomenadione (Vit K) 1-5 mg PO using IV prep is indicated
Sumatriptan
- Doses (PO, SC, Intranasal)
- CIs, Cautions
- SEs
- Pregnancy
-
Dose:
- PO 50-100 mg for 1 dose, followed by 50-100 mg after at least 2 hrs if required
- SC 3-6 mg for 1 dose, followed by 3-6 mg after at least 1 hr if required
- Intranasal 10-20 mg in one nostril, again after at least 2 hrs if required
- CIs: IHD, mild uncontrolled HTN, mod-sev HTN, peripheral vascular disease, previous cerebrovascular accident, previous MI, previous TIA, Prinzmetal’s angina
- Cautions: Predisposing coronary artery disease factors, elderly, Hx of seizures, mild controlled HTN, risk factors for seizures
- SEs: Dizziness, drowsiness, dyspnoea, flushing, myalgia, nausea, vomiting, pain, skin reactions, temp sensation altered
- Pregnancy: best to avoid if possible due to limited evidence
- Consider dose reduction to 25–50 mg in mild to moderate hepatic impairment
Propranolol
- Dose
- CIs and cautions
- SEs
- Dose: 80 - 240 mg daily in divided doses
- CIs: Asthma, COPD, hypotension, bradycardia, metabolic acidosis, 2nd or 3rd degree AV block, severe peripheral arterial disease, sick sinus syndrome, uncontrolled HF, pheochromocytoma, Prinzmetals angina
- Cautions: DM, myasthenia gravis, portal hypertension, psoriasis, may mask hypoglycaemia or thyrotoxicosis
- Elderly STOPP criteria:
- In combo with verapamil or diltiazem
- With bradycardia (HR<50bpm)
- DM with frequent hypoglycaemia episodes
- History of asthma requiring
- Elderly STOPP criteria:
- SEs: abdo discomfort, confusion, depression, diarrhoea, dizziness, dry eye, dyspnoea, erectile dysfunction, fatigue, headache, HF, nausea, paraesthesia, PVD, rash, sleep disorder, syncope, visual impairment, vomiting
Topiramate
- Dose: 50 - 100 mg daily, two divided doses, taken at night. Start with 25 mg OD for 1 week, increased in steps of 25 mg each week, max 200 mg daily
- ENZYME INDUCER
- Risk of suicidal thoughts and behaviour
- Cautions: acute porphyria’s, risk of metabolic acidosis
- Pregnancy: Use of highly effective contraception and fully informed of risks or avoid altogether
- Breastfeeding: AVOID
- Renal impairment: half dose if creatinine clearance < 70
Drug-induced liver injury (8 drug causes)
-
Flucloxacillin and Co-Amoxiclav
- Cholestatic hepatitis and jaundice
- Idiosyncratic, not dose-related
- Onset may be delayed for up to 2 months following Tx
-
Paracetamol
- Causes a dose-dependent acute liver injury → can lead to acute liver failure
-
NSAIDs
- Idiosyncratic hepatitis, resolves in most cases after the termination of drug therapy
- Classically causes a cholestatic hepatitis
- Aspirin can also cause hepatitis but tends to be dose-related
-
Anti-TB drugs (RIPE)
- Can cause liver injury
-
Methotrexate
- Severe fibrosis and cirrhosis if not adequately monitored
-
Amiodarone
- Steato hepatitis
- Statins: can cause a mild transaminitis (raise in AST/ALT), monitor LFTs in those with mild liver disease
Typical dose of:
Paracetamol
0.5 - 1 kg QDS
Typical dose of:
Ibuprofen
200- 400 mg TDS
Typical dose of:
Codeine
30 - 60 mg QDS
Typical dose of:
Co-codamol
2 tabs QDS
Typical dose of:
Cyclizine
50 mg TDS
Typical dose of:
Metoclopramide
10 mg TDS
Typical dose of:
Amoxicillin
500 mg TDS
Typical dose of:
Clarithromycin
500 mg BD
Typical dose of:
Lansoprazole
15-30 mg OD
Typical dose of:
Omeprazole
20-40 mg OD
Typical dose of:
Aspirin
75-300 mg OD
Typical dose of:
Clopidogrel
75-300 mg OD
Typical dose of:
Atenolol
25-100 mg OD
Typical dose of:
Ramipril
1.25-10 mg OD
Typical dose of:
Furosemide
20 mg OD to 80 mg BD
Typical dose of:
Amlodipine
5-10 mg OD
Typical dose of:
Levothyroxine
25-200 micrograms OD
Typical dose of:
Metformin
500 mg OD to 1 g BD
Typical dose of:
Atorvastatin
10-80 mg OD (at night)
Typical dose of:
Simvastatin
10-40 mg OD (at night)
Drugs that lower seizure threshold (8)
- Alcohol/cocaine/amphetamines
- Quinolones: ciprofloxacin, levofloxacin
- Aminophylline and theophylline
- Bupropion
- Methylphenidate (ADHD med)
- Mefenamic acid
- P450 Inducers / inhibitors
- Withdrawal of benzos, baclofen, hydroyzine
Drugs not administered daily? (7)
- Bisphosphonates: Weekly (Can be daily or monthly too)
- Hydroxocobalamin: 2-3 monthly
- Injectable antipsychotics: Weekly-monthly
- Methotrexate: Once a week
- Injectable RA drugs: Every 2 weeks
- Goserelin: 3 monthly
- Implants: 3 monthly
Presentation of rhabdomyolysis
- Muscle swelling and tenderness
- Weakness
- Grey/brown urine
- Raised CK
May lead to: - Renal failure
- Hyperkalaemia
What can increase risk of rhabdomyolysis?
STATINS plus:
- older age
- female
- genetics
- renail impairment
- concomitant diltiazem (max statin dose = 20 mg)
Tx of rhabdomyolysis
- IV fluids
- Consider sodium bicarb
- Monitor K+
Known teratogenics (10)
- ACE-Is and ARBs
- Antiepileptics, e.g. valproate, carbamazepine, phenytoin
- Cytotoxic agents
- Sex hormones
- Statins
- Lithium salts
- Thalidomide
- Warfarin
- Retinoids
- Abx - tetracyclines, trimethoprim, quinolones, aminoglycosides, sulphonamides
- Sulfonylureas
Gentamicin monitoring
Multiple daily dose:
- Peak (1hr post dose): 3-5 mg/litre
- Trough (pre next dose): < 1 mg/litre
If peak is high: decrease dose
If trough is high: increase intervals
Once daily dose:
- 6-14 hrs after start of infusion
- Targets concentration < 1 mg/litre
Warfarin strengths and tablet colours
500 micrograms - White
1 mg - Brown
3 mg - Blue
5 mg - Pink
Typical dose of:
Warfarin
1 mg - 15 mg (average = 5 mg)
OD, same time each day, usually evening
Drugs that should be avoided in HF?
- Thiazolididiones (e.g. pioglitazone)
- Verapamil/Dialtezam
- NSAIDs/glucocorticoids (fluid retention)
- Class I antiarrhythmics (flecainide, lidocaine, quinidine)
Cytochrome P450
Substrates (8)
- Warfarin
- COCP
- Statins
- Nifedipine
- Theophylline
- Tricyclics
- Corticosteroids
- Pethidine
Cytochrome P450
Inducers (10)
GPRS Cell Phone (Inducer = electric = phone)
- Griseofulin
- Phenytoin
- Rifampicin
- Sulfonylureas
- Carbamazepine
- Phenobarbitone
- Topiramate
- Smoking
- St John’s Wort
- Alcohol - CHRONIC
Cytochrome P450
Inhibitors (12)
SICKFACES.COM (Inhibitor = inhibit getting better = sick)
- Sodium Valproate
- Isoniazid
- Cimetidine
- Ketoconazole
- Fluconazole/Miconazole
- Acute alcohol, grapefruit juice
- Chloramphenicol
- Erythromycin
- Sulfonamides
- Ciprofloxacin
- Omeprazole
- Methotrexate
Monitoring Requirements
Levothyroxine
- Annual TFTs if on maintenance
- After dose adjustment -> wait 6/8 weeks then check TFTs
- Acute illness may affect results
Monitoring Requirements
Amiodarone
- TFTs before Tx and every 6 months after
- Associated with both hypo- and hyper- thyroidism
Monitoring Requirements
Digoxin
- Heart rate monitored before administration
Monitoring Requirements
Gentamicin
- Narrow therapeutic window -> plasma concentration
Monitoring Requirements
Methotrexate
Before, every 1-2 weeks unstable, 2-3 months after:
- FBC (neutropenia), including ESR
- LFTs
- Renal function
Baseline CXR and then if pulmonary toxicity occurs
Monitoring Requirements
Adalimumab
- Evaluate for active/inactive TB
- If prev treated for TB, monitor every 3 months for recurrence
Monitoring Requirements
Carbamazepine
- FBC (neutropenia) - look out for SORE THROAT
Monitoring Requirements
Clozapine
- FBCs - leucocytes and differential blood counts
- WCC monitoring weekly for 18 weeks, then fortnightly for 1 year, then monthly
- Close medical supervision during initiation (risk of hypotension and convulsions)
- Lipids and weight at baseline, frequent intervals during first 3 months, 3 monthly for one year, then yearly
- Fasting blood glucose at baseline, 4-6 months then annually
Monitoring Requirements
Lithium
Serum-lithium concentration (0.4 - 1 mmol/litre)
- Higher end in acute treatment
- Measure 12 hr post dose after at least 4 days
- Measure weekly until stabilised
- Measure every 3 months thereafter
- Cardiac function regularly
- TFTs, renal function, calcium and BMI every 6 months
Lithium
Adverse effects
- Fine hand tremor
- Nausea
- Weight gain
- Metallic taste
- Mild polydipsia
- Polyuria
- Alteration of renal function
- Diabetes insipidus
- Hyperparathyroidism
- Hyperthyroidism
Lithium
Toxicity
- Severe hand tremor
- Vomiting and diarrhea
- Blurred vision
- Muscle weakness
- Ataxia
- Dysarthria
- Confusion
- Nystagmus
- Renal failure
- Seizures
- Coma
Lithium
Interactions
ACE-I - increases conc
Diuretics - hypokalaemia and increases concs
NSAIDs - increases concs
Sodium-containing compounds - decreases concs
Acetylcysteine indications in paracetamol overdose
- There is a staggered overdose* or there is doubt over the time of paracetamol ingestion, regardless of the plasma paracetamol concentration; or
- The plasma paracetamol concentration is on or above a single treatment line joining points of 100 mg/L at 4 hours and 15 mg/L at 15 hours, regardless of risk factors of hepatotoxicity
- > 150 mg/kg