Pharmacology Flashcards
Azathioprine
Class: anti-proliferative agent.
MOA: inhibits purine synthesis —> inhibiting DNA and RNA replication.
Indication: transplant immunosuppression, RA, IBD.
Side effects/contraindications: bone marrow suppression.
Cyclophosphamide
Class: anti-proliferative agent/bifunctional alkylating agent.
MOA: DNA cross linking —> inhibiting protein synthesis.
Indication: immune based renal disease, chemotherapy, autoimmune and CT disorders.
Side effects/contraindications: bone marrow suppression.
Ciclosporin
Class: calcineurin inhibitor.
MOA: inhibit pro-inflammatory cytokine synthesis, such as IL-2 —> suppressing T cell activation and differentiation.
Indication: transplant immunosuppression.
Side effects: everything is increased - fluid, BP, K+, hair, gums, glucose.
Tacrolimus
Class: calcineurin inhibitor.
MOA: inhibit pro-inflammatory cytokine synthesis, such as IL-2 —> suppressing T cell activation and differentiation.
Indication: transplant immunosuppression.
Side effects/contraindications: increased risk of infection.
Trimethoprim
Class: antibiotic.
MOA: inhibits folate synthesis —> inhibiting nucleic acid synthesis.
Indication: UTI.
Side effects/contraindications: GI upset and skin rash. Avoid in first trimester and folate deficiency.
Nitrofurantoin
Class: antibiotic.
MOA: active metabolite damages bacterial DNA causing cell death.
Indication: UTI.
Side effects/contraindications: GI upset and hypersensitivity reactions. Avoid in pregnancy, babies < 3 months old and renal impairment.
Co-amoxiclav
Class: penicillins.
MOA: inhibit bacterial cell wall synthesis.
Indication: pyelonephritis.
Side effects/contraindications: D+V.
Ciprofloxacin
Class: fluoroquinolone.
MOA: inhibits DNA gyrase —> inhibiting DNA replication.
Indication: pyelonephritis.
Gentamicin
Class: aminoglycoside.
MOA: inhibits 30S ribosomal subunit —> inhibiting protein synthesis.
Indication: serious gram -ve infections e.g. pyelonephritis, sepsis and meningitis.
Side effects/contraindications: Ototoxicity and nephrotoxicity. Avoid in myasthenia gravis.
Cefalexin
Class: cephalosporins.
MOA: bind penicillin binding proteins —> inhibiting bacterial cell wall synthesis.
Indication: pyelonephritis.
Side effects/contraindications: GI upset. Use cautiously in people at risk of C.diff infection.
Ramipril, lisinopril, perindopril
Class: angiotensin-converting enzyme inhibitor (ACEi).
MOA: preventing the conversion of angiotensin 1 to angiotensin 2, this inhibits vasoconstriction and suppresses aldosterone secretion.
Indication: reduce proteinuria in glomerulonephritis and CKD. Anti-hypertensive, HF, IHD.
Side effects/contraindications: first dose hypotension, persistent dry cough and hyperkalaemia. Avoid in patients with renal artery stenosis and AKI, also in pregnancy.
Losartan, candesartan, irbesartan
Class: angiotensin receptor blockers (ARBs).
MOA: block action of angiotensin 2 on the angiotensin type 1 receptor, inhibiting vasoconstriction and suppressing aldosterone secretion.
Indication: reduce proteinuria in glomerulonephritis and CKD. Anti-hypertensive, HF, IHD.
Side effects/contraindications: first dose hypotension, hyperkalaemia and renal failure. Avoid in patients with renal artery stenosis and AKI, as well as pregnancy.
Furosemide, bumetanide
Class: loop diuretic.
MOA: inhibits Na+/K+/2Cl- cotransporter on TAL —> decreasing Na+ and water reabsorption.
Indication: pulmonary oedema, fluid overload (HF, renal disease or liver failure).
Side effects/contraindications: dehydration and hypotension. Avoid in patients with dehydration and hypovolaemia.
Oxybutinin, tolterodine
Class: anti-muscarinic.
MOA: inhibits binding of ACh to M3 receptor —> stimulating bladder relaxation.
Indication: overactive bladder and urge incontinence.
Side effects/contraindications: dry mouth, tachycardia, constipation, blurred vision, urinary retention. Avoid in UTIs.
Mirabegron
Class: beta 3 adrenergic agonist.
MOA: activates beta 3 receptors relaxing detrusor smooth muscle.
Indication: overactive bladder and urge incontinence.
Side effects/contraindications: avoid in uncontrolled hypertension.
Doxazosin, tamsulosin, alfuzosin
Class: alpha blocker (alpha 1 adrenoceptor antagonist).
MOA: inhibit alpha 1 receptors —> SM relaxation in prostate —> reduced resistance to bladder outflow. Also causes vasodilation causing BP to fall.
Indication: BPH (1st line). Add-on in resistant hypertension.
Side effects/contraindications: postural hypotension, dizziness and syncope.
Dutasteride, finasteride
Class: 5 alpha reductase inhibitors.
MOA: inhibit 5 alpha reductase —> inhibiting conversion of testosterone to DHT —> reduces prostatic enlargement. Takes several months to work.
Indication: BPH (2nd line).
Side effects/contraindications: impotence, reduced libido, gynaecomastia. Pregnant women shouldn’t handle these drugs.
Sildenafil, tadalafil
Class: phosphodiesterase type 5 inhibitors.
MOA: inhibits PDE-5 —> prevention of cGMP breakdown, increasing its concentrations —> SM relaxation and vasodilation —> penile blood flow and erection (sexual stimulation required).
Indication: erectile dysfunction.
Side effects/contraindications: flushing, headaches, dizziness, nasal congestion. Serious = hypotension, tachycardia, palpitations, priapism.
Alprostadil
Class: synthetic prostaglandin E1 analogue.
MOA: induces vascular SM relaxation —> erection.
Indication: erectile dysfunction.
Cisplatin
Class: platinum based chemotherapy.
MOA: alkylating agent —> cross-linking —> DNA damage.
Indication: bladder cancer, metastatic testicular cancer and metastatic ovarian cancer.
Insulin aspart (rapid-acting), insulin glargine (long-acting), biphasic insulin (mixture of rapid- and intermediate-acting), soluble insulin (short-acting)
Class: insulin formulations.
MOA: stimulates glucose uptake into skeletal muscle and fat, stimulates glycogenesis and lipogenesis, inhibits gluconeogensis and ketogenesis. Drives K+ into cells.
Indication: insulin replacement for T1D, control of blood glucose in T2D, diabetic emergencies e.g. DKA and HHS, alongside glucose in hyperkalaemia.
Side effects/contraindications: hypoglycaemia, lipohypertrophy.
Gliclazide, glimepiride
Class: sulfonylurea.
MOA: stimulates pancreatic insulin secretion via blocking K+ channels in beta cell causing depolarisation and opening of voltage gated Ca2+ channels.
Indication: T2D.
Side effects/contraindications: GI upset, hypoglycaemia, weight gain.
Repaglinide
Class: meglitinides.
MOA: stimulates insulin secretion.
Indication: T2D.
Side effects/contraindications: GI upset, hypoglycaemia.