Drugs Flashcards
P450 Enzyme inhibitors
Sodium valproate Ketoconazole Isoniazid Amiodarone Chloramphenicol Erythromycin Quinidine Grapefruit juice
Ketoconazole
Antifungal medication.
An imidazole derivative which acts as a potent inhibitor of cortisol and aldosterone synthesis by inhibiting the activity of 17α-hydroxylase, 11-hydroxylation steps and at higher doses the cholesterol side-chain cleavage enzyme.
It also inhibits the activity of adrenal C17-20 lyase enzymes resulting in androgen synthesis inhibition, and may have a direct effect on corticotropic tumour cells in patients with Cushing’s disease.
Endogenous Cushing’s syndrome; Tinea pedis; treatment and prophylaxis of seborrhoeic dermatitis and dandruff; Treatment and prophylaxis of pityriasis versicolor; Vaginal and vulva candidiasis.
Risk of hepatotoxicity associated with oral ketoconazole is greater than the benefit in treating fungal infections (doesn’t include Cuishings).
The use of carbonated drinks, such as cola, improves ketoconazole bioavailability.
S/E: Skin reactions. P450 enzyme inhibitor
Avoid in pregnancy / breastfeefing / hepatic imparement.
Monitor ECG before and one week after initiation
Cyclizine
An antiemetic.
Nausea, vomiting, vertigo, motion sickness, labyrinthine disorders, palliative care.
Although not licenced for morning sickness it is considered useful and safe.
Cautions: Epilepsy; glaucoma; prostatic hypertrophy; severe heart failure, mean arterial pressure and pulmonary wedge pressure; susceptibility to angle-closure glaucoma; urinary retention
S/E: Agitation; angle closure glaucoma; depression
Drowsiness may affect performance of skilled tasks; effects of alcohol enhanced
Ondansetron
Antiemetic. Specific 5HT3-receptor antagonist which blocks 5HT3 receptors in the gastro-intestinal tract and in the CNS.
Emetogenic chemotherapy or radiotherapy; postoperative nausea and vomiting.
C/I: long QT syndrome.
S/E: Constipation; feeling hot; headache; sensation abnormal
Small risk of cleft lip and/or cleft palate in babies born to women who used oral ondansetron during the first trimester of pregnancy.
Metoclopramide hydrochloride
Antiemetic.
Brand name: Maxolon
Treats nausea and vomiting associated with: chemo, RT, migraine, post-operatively.
Palliative care - hiccup; nausea and vomiting.
C/I: 3–4 days after GI surgery; epilepsy; GI haemorrhage; GI obstruction; GI perforation; phaeochromocytoma, parkinsons.
S/E: Asthenia; depression; diarrhoea; drowsiness; hypotension; menstrual cycle irregularities; movement disorders; parkinsonism (extrapyramidal SE)
Can induce acute dystonic reactions involving facial and skeletal muscle spasms and oculogyric crises.
Safe in pregnancy one of the second line options after pyridoxine / doxylamine.
Antiemetics
Metoclopramide Cyclizine Ondansetron Prochlorperazine (typical antipsychotic) Domperidone Hyoscine hydrobromide Metoclopramide hydrochloride Trifluoperazine (typical antipsychotic) Haloperidol (typical antipsychotic)
Terlipressin acetate
Analogue of vasopressin.
Bleeding from oesophageal varices;
Cautions: Arrhythmia; elderly; electrolyte and fluid disturbances; heart disease; history of QT-interval prolongation; respiratory disease; septic shock; uncontrolled hypertension; vascular disease
S/E: Abdominal cramps; arrhythmias; diarrhoea; headache; hypertension; hypotension; pallor; peripheral ischaemia; vasoconstriction
Diltiazem hydrochloride
Non-dihydropyridine calcium channel blocker.
Prophylaxis and treatment of angina; hypertension; Chronic anal fissure (unlicenced).
C/I : Acute porphyrias ; cardiogenic shock; heart failure; left ventricular failure with pulmonary congestion; second- or third-degree AV block; severe bradycardia; sick sinus syndrome; significant aortic stenosis; Cardiac conduction disorders; constipation; gastrointestinal discomfort; malaise
Overdose: nausea, vomiting, dizziness, agitation, confusion, and coma in severe poisoning
There is some evidence that sudden withdrawal of calcium-channel blockers may be associated with an exacerbation of myocardial ischaemia.
Beta blockers / β-Adrenergic Antagonists
Metoprolol, Atenolol, Propranolol, Sotalol
Hypertension
Timolol, betaxolol - glaucoma (reduces aqueous production)
C/I: Asthma; cardiogenic shock; hypotension; marked bradycardia; metabolic acidosis; phaeochromocytoma (apart from specific use with alpha-blockers); Prinzmetal’s angina; second-degree AV block; severe peripheral arterial disease; sick sinus syndrome; third-degree AV block; uncontrolled heart failure
S/E: Abdominal discomfort; bradycardia; confusion; depression; diarrhoea; dizziness; dry eye (reversible on discontinuation); dyspnoea; erectile dysfunction; fatigue; headache; heart failure; nausea; paraesthesia; peripheral coldness; peripheral vascular disease; rash (reversible on discontinuation); sleep disorders; syncope; visual impairment; vomiting
Ipratropium bromide
Anticholinergics (inhaled) - bronchodilator.
Reversible airways obstruction (asthma and COPD); Acute bronchospasm; Severe or life-threatening acute asthma; Rhinorrhoea associated with allergic and non-allergic rhinitis.
Cautions: Bladder outflow obstruction; paradoxical bronchospasm; prostatic hyperplasia; susceptibility to angle-closure glaucoma.
S/E: Arrhythmias; cough; dizziness; dry mouth; headache; nausea; Gastrointestinal motility disorder; throat complaints
It is used by inhaler or nebulizer.
Bleomycin
Glycopeptide antibiotic - cancer medication
Squamous cell carcinoma; Metastatic germ cell cancer; Non-Hodgkin’s lymphoma
C/I: Acute pulmonary infection; significantly reduced lung function
S/E: Alopecia; angular stomatitis; appetite decreased; chills; fever; haemorrhage; headache; interstitial pneumonia; leucopenia; malaise; nail discolouration; nail disorder; nausea; pain; pulmonary fibrosis; scleroderma; skin reactions; stomatitis; vomiting; weight decreased
Treatment of lymphoma (4 drugs)
Dacarbazine, vinblastine, bleomycin, and doxorubicin
Non-nucleoside reverse transcription inhibitors (NNRTI)
HIV antiviral drugs
Nevirapine, Efavirenz, Rilpivirine
S/E stephen johnson syndrome, hepatitis
Efavirenz, Nevirapine.
HIV infection in combination with other antiretroviral drugs
Integrase strand transfer inhibitors (InSTIs)
HIV antiviral drugs
Dolutegravir, Raltegravir, elvitegravir
S/E GI upset, insomnia
Dolutegravir
Integrase strand transfer inhibitors (InSTIs).
Preferred HIV Drug recommended by WHO.
S/E: Anxiety; depression; diarrhoea; dizziness; fatigue; flatulence; gastrointestinal discomfort; headache; nausea; skin reactions; sleep disorders; vomiting
Teratogenic (neural tube defects)
Amoxicillin
Penicillin antibiotic.
Broader spec. than penicillin.
Streps, meningococcus, syphilis, gram -ve rods.
Community-acquired pneumonia; Acute exacerbation of bronchiectasis / COPD; Lyme disease; Anthrax; Dental abscess; Listerial meningitis; sinusitis, salmonellosis; Endocarditis; Helicobacter pylori eradication; Acute diverticulitis; Prophylaxis and treatment of urinary-tract infection.
Cautions: allergy; Acute lymphocytic leukaemia; chronic lymphocytic leukaemia; cytomegalovirus infection; glandular fever; maintain adequate hydration with high doses.
S/E: Diarrhoea; hypersensitivity; nausea; skin reactions; thrombocytopenia; vomiting
Penicillin based antibiotics
B-lactams (Inhibition of cell wall synthesis).Effective mostly againstGram-positivebacteria.
Amoxicillin, flucloxacillin, benzylpenicillin (penicillin)
The penicillins are bactericidal and act by interfering with bacterial cell wall synthesis. They diffuse well into body tissues and fluids, but penetration into the cerebrospinal fluid is poor except when the meninges are inflamed. They are excreted in the urine in therapeutic concentrations.
S/E: Diarrhoea; hypersensitivity; nausea; skin reactions; thrombocytopenia; vomiting
The most important side-effect of the penicillins is hypersensitivity which causes rashes and anaphylaxis and can be fatal. Allergic reactions to penicillins occur in 1–10% of exposed individuals; anaphylactic reactions occur in fewer than 0.05% of treated patients. Patients with a history of atopic allergy (e.g. asthma, eczema, hay fever) are at a higher risk of anaphylactic reactions to penicillins. Individuals with a history of anaphylaxis, urticaria, or rash immediately after penicillin administration are at risk of immediate hypersensitivity to a penicillin; these individuals should not receive a penicillin.
Individuals with a history of a minor rash (i.e. non-confluent, non-pruritic rash restricted to a small area of the body) or a rash that occurs more than 72 hours after penicillin administration are probably not allergic to penicillin and in these individuals a penicillin should not be withheld unnecessarily for serious infections; the possibility of an allergic reaction should, however, be borne in mind. Other beta-lactam antibiotics (including cephalosporins) can be used in these patients.
Flucloxacillin
Penicillin based antibiotic
Staphylococci (Gram +ve b-lactamase producers)
Infections due to beta-lactamase-producing staphylococci including otitis externa; Adjunct in pneumonia; Adjunct in impetigo; Cellulitis; Erysipelas; Diabetic foot infection; Leg ulcer infection; Endocarditis; Osteomyelitis; Surgical prophylaxis; Prevention of Staphylococcus aureus lung infection in cystic fibrosis.
S/E: Diarrhoea; hypersensitivity; nausea; skin reactions; thrombocytopenia; vomiting; gastrointestinal disorder
Patients who are allergic to one penicillin will be allergic to all.
Co-amoxiclav
Penicillin based antibiotic.
Amoxicillin + clavulanic acid.
Infections due to beta-lactamase-producing strains (where amoxicillin alone not appropriate), including respiratory tract infections, bone and joint infections, genito-urinary and abdominal infections, and animal bites; diabetic foot infection; Leg ulcer infection; Cellulitis; Erysipelas; Surgical prophylaxis; Community-acquired pneumonia; Hospital-acquired pneumonia; Acute exacerbation of bronchiectasis / COPD; sinusitis; otitis media; Acute pyelonephritis;
Urinary-tract infection.
C/I: History of co-amoxiclav/ penicillin associated jaundice or hepatic dysfunction.
Cautions: Increased risk of erythematous rashes in acute lymphocytic leukaemia, chronic lymphocytic leukaemia, cytomegalovirus infection, glandular fever; maintain adequate hydration with high doses (particularly during parental therapy); Cholestatic jaundice can occur
S/E: C.diff infeciton,
The 4 Cs
clindamycin, cephalosporins, co-amoxiclav and ciprofloxacin
Cephalosporins
B-lactams (Inhibition of cell wall synthesis). Effective mostly againstGram-positivebacteria.
Active against staphs (including b-lactamase producers), streps, pneumococci, E Coli etc.
Used mainly in surgical prophylaxis or for UTI, pneumonia etc if penicillin allergic (10% will also be cephalosporin allergic).
S/E Hypersensitivity, warfarin potentiation, Abdominal pain; diarrhoea; dizziness; eosinophilia; headache; leucopenia; nausea; neutropenia; skin reactions; thrombocytopenia; vomiting; vulvovaginal candidiasis
C. diff infection!
Cefotaxime, cefuroxime, ceftriaxone
Glycopeptides
Inhibition of cell wall synthesis.
Only act on gram +ve organisms (cannot penetrate wall of gram -ve). Not absorbed from the GI tract and are only given parenterally.
e.g. vancomycin (!toxic), teicoplanin
Aminoglycosides
Inhibition of Protein Synthesis.
Treat serous gram -ve infection.
e.g. gentamicin (toxic)
Families of antibiotics
- Penicillins and cephalosporins (B-lactams)
- Glycopeptides
- Aminoglycosides
- Macrolides
- Tetracyclines
- Oxazolidinones
- Cyclic lipopeptide
- Fluoroquinolones