Top 100 Drugs Flashcards
Side Effects - Sodium Valporate
Valproate
Appetite increase, so weight gain
Liver failure (monitor LFTs during 1st 6 months)
Pancreatitis
Reversible hair loss (grows back curly, apparently)
Oedema
Ataxia
Teratogenicity, Tremor, Thrombocytopaenia
Encephalopathy (due to hyperammonaemia) / Enzyme inducer
Has the greatest risk of fetal abnormalities
Indications - Sodium Valporate
Seizure prophylaxis in epilepsy
Manic episodes in bipolar disorder - used as prophylaxis against recurrence
Contraindications - Sodium Valporate
Women of child-bearing age - especially time of conception and pregnancy
Hepatic Impairment
Renal impairment
Aminosalicylates - Indications
Mesalazine - 1st line mild/moderate UC
Sulfasalazine - Used with a DMARD in rheumatoid arthritis
Side Effects - Aminosalicylates
Nausea
Dyspepsia
Headache
Blood Abnormalities - leucopenia and thrombocytopenia (rare)
Oligospermia
Can cause severe hypersensitivity reactions
Contraindications - Aminosalicylates
Not given to those with aspirin hypersensitivity
Mesalazine - pH sensitive coating - affected by PPIs and Lactulose
PPI - Indications
Peptic ulcer disease
NSAID-associated ulcers
Symptomatic relief of dyspepsia and GORD
H. pylori infection
PPI - Mechanism
Irreversibly inhibit H+/K+ ATPase in gastric parietal cells
Suppress gastric acid production almost completely
PPI - Adverse effects
GI disturbances
Headache
Prolonged treatment - hypomagnesaemia - severe can lead to tetany
PPI - Warnings
May disguise symptoms of gastro-oesophageal cancer
Cautioned in those with osteoporosis - increased risk of fracture
PPI - Interactions
Reduce antiplatelet affect of clopidogrel by decreasing its activation of cytochrome P450 enzymes
Metronidazole - Indications
Antibiotic-associated colitis - gram-positive anaerobe Clostridium difficile
Oral Infections / Aspiration pneumonia
Surgical and gynae infections by gram-negative anaerobes
Protozoal infections - trichomonal vaginal infection, amoebic dysentery and giardiasis
Metronidazole - Mechanism
Anaerobic Bacteria - DNA degradation and cell death (bactericidal)
Metronidazole - Adverse Effects
GI upset (nausea and vomiting)
Delayed Hypersensitivity reactions -
Can cause peripheral and optic neuropathy, seizures and encephalopathy
Metronidazole - Warnings
Metabolised by P450 enzymes - reduced in people with severe liver disease
Inhibits acetaldehyde dehydrogenase - responsible for clearing alcohol metabolite
Alcohol should not be drunk while taking metronidazole
Metronidazole - Interactions
Some inhibitory effect on CYP enzymes
Reduction in warfarin metabolism and phenytoin
Cephalosporins - examples?
Ceftriaxone, Cefalexin, Meropenem, Ertapenem
Ceftriaxone - Mechanism
3rd generation cephalosporin
Broad-spectrum - long half-life
Penetrates the meninges, eyes and inner ear
Used in the treatment of bacterial infections caused by susceptible usually gram-positive
Ceftriaxone works by inhibiting the mucopeptide synthesis in the bacterial cell wall
Prevents them from maintaining an osmotic gradient leading to bacterial cell swelling and death
Has in vitro activity against gram-positive aerobic, gram-negative aerobic, and anaerobic bacteria
Bactericidal activity of ceftriaxone results from the inhibition of cell wall synthesis and is mediated through ceftriaxone binding to penicillin-binding proteins (PBPs)
Ceftriaxone is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended-spectrum beta-lactamases
Ceftriaxone - Cautions
Ceftriaxone should not be mixed with or giving in the same IV line as diluents/products containing calcium as they may cause ceftriaxone to precipitate.
In those at increased C. difficile infection
Epilepsy
Cautioned in those with renal impairment
Ceftriaxone - Adverse Effects
Ceftriaxone use may also cause biliary sludge or gallbladder pseudolithiasis.
GI upset
Antibiotic associated colitis -> can lead to bowel perforation and death
Clostridium difficile infections
Hypersensitivity -> Cross-reactivity can occur in penicillin allergic patients
Ceftriaxone - Interactions
Enhance anticoagulant effects of warfarin by killing normal gut flora that synthesise vitamin K
Increase nephrotoxicity of aminoglycosides
Reduce conc. of valproate
Methotrexate - Mechanism
DMARD for rheumatoid arthritis
Chemotherapy regimen for cancers: leukaemia, lymphoma and some solid tumours
Treatment of severe psoriasis
Mechanism of action
Folic analogue inhibits dihydrofolate reductase (which converts dietary folate to tetrahydrofolate -needed for DNA synthesis) and thymidylate synthase - reduce production of thymine needed for DNA synthesis –> prevents cellular replication
Anti-inflammatory and immunosuppressive - inhibition of inflammatory mediators IL-6, IL-8 and TNF-alpha
Reduction in methionine
Methotrexate - Adverse Effects
Mucosal damage
Bone marrow suppression (can lead to neutropenia and increased infection risk)
Hypersensitivity reactions - cutaneous reactions, hepatitis, pneumonitis
Long term can lead to hepatic cirrhosis or pulmonary fibrosis
Renal failure and hepatic toxicity
Risk of accidental overdose - treated with folinic acid which rescues normal cells from methotrexate effects along with hydration and urinary alkalinisation - enhance excretion
Methotrexate - Contraindicated
Teratogenic - avoided in pregnancy (both men and women)
Severe renal impairment
Abnormal liver function
Methotrexate - Interactions
Toxicity likely with drugs that can inhibit its renal excretion - NSAIDs, penicillins
Co-prescription with other folate antagonists (Trimethoprim and phenytoin) can lead to haematological abnormalities
Dexamethasone (Glucocorticoids - systemic corticosteroids) - Mechanism
Used to treat allergic or inflammatory disorders
Suppression of autoimmune disease
Cancer treatment as part of chemotherapy or to reduce tumour associated swelling
Hormone replacement in adrenal insufficiency or hypoparathyroidism
Mechanism of Action
Bind to the glucocorticoid receptor - inhibiting pro-inflammatory signals (cytokines and TNF-alpha) and promoting anti-inflammatory signals
Decreased vasodilation and permeability of capillaries
Suppression of circulating monocytes and eosinophils
Gluconeogenesis from increased circulating fatty acids and amino released by fat and muscle catabolism
Mineralocorticoid effect - Na+ retention and K+ excretion
Dexamethasone (Glucocorticoids - systemic corticosteroids) - Adverse Effects
Immunosuppression - increases the risk and severity of infection - alters host response
Increased catabolism - proximal muscle weakness, skin thinning with easy bruising and gastritis
Mood and behavioural changes - insomnia, confusion, psychosis
Hypertension, hypokalaemia and oedema
Suppresses ACTH production - in prolonged treatment leads to adrenal atrophy
If steroids are withdrawn too quickly - Addisonian crisis
Needs to be withdrawn slowly by can cause symptoms of chronic glucocorticoid deficiency
Cannot produce cortisol secretion in response to stress - needs to be provided artificially in acute illness (double dose)
Dexamethasone (Glucocorticoids - systemic corticosteroids) - Contraindicated
§ Those with infection
§ Children
Dexamethasone (Glucocorticoids - systemic corticosteroids) - Interactions
Peptic ulcers and GI bleeding - especially if used with NSAIDs
Hypokalaemia enhancement with those on Beta-2 agonists, theophylline (PDE inhibitor), loop and thiazide diuretics
Efficacy reduced by cytochrome P450 inducers (phenytoin, carbamazepine, rifampcin)
Calcium Gluconate - Indications
Used in beta blocker and Calcium Channel Toxicity
Severe acute hypocalcaemia or hypocalcaemic tetany
Acute severe hyperkalaemia (plasma-potassium concentration above 6.5 mmol/litre or in the presence of ECG changes)
Calcium deficiency, Mild asymptomatic hypocalcaemia
Hyperkalaemia is common among hospital inpatients
First line emergency treatment for severe hyperkalaemia associated with ECG abnormalities
Calcium Gluconate - Dosage
10mL of calcium gluconate 10% IV over 10-15 minutes
Calcium Gluconate - Mechanism of Action
○ In hyperkalaemia - calcium raises the myocardial threshold potential, reducing excitability and the risk of arrhythmias - no effect on serum potassium
Calcium Gluconate -Contraindicated
Conditions associated with hypercalcaemia (e.g. some forms of malignant disease)
Allopurinol - Indications
Prevent recurrent attacks of gout
Thiazide or loop diuretics - increases serum uric acid
Aspirin inhibits renal excretion of uric acid
Drug-induced gout C
Prevent uric acid and calcium oxalate renal stones
Prevent hyperuricaemia and tumour lysis syndrome
Allopurinol - Mechanism of Action
Xanthine oxidase inhibitor
Xanthine oxidase metabolises xanthine from purines to uric acid