Medication GP Flashcards
DPP4 inhibitors - MOA, agents, side effects
MOA: DPP4 inhibitor - increases endogenous incretin effect by inhibiting DPP4 that breaks down GLP-1, causing increased insulin secretion, decreased glucagon secretion, delayed gastric emptying. Used to treat T2DM
Agents: Linagliptin (trajgenta), sitagliptin, saxagliptin, alogliptin
Side effects: Diarrhoea, constipation, urinary infections, worsening renal function, increased satiety
SNRI - Class, MOA, agents, indications, side effects
Class: antidepressant
MOA: Inhibit serotonin and noradrenaline reuptake
in synaptic cleft, increasing serotonin and noradrenaline levels
Agents: duloxetine, venlafaxine, milnacipran
Indications: MDD, GAD, neuropathic pain, (with milnacipran) fibromyalgia, stress incontinence in women
Side effects: Insomnia, strange dreams, nightmares, increased BP, GI upset, SIADH, sexual dysfunction, increased cholesterol and triglycerides
SSRI - Class, MOA, agents, indications, side effects
Class: Antidepressant
MOA: Inhibit the presynaptic reuptake of serotonin (5-hydroxytryptamine, 5HT), increasing serotonin levels
Agents: Fluoxetine, paroxetine, sertraline, citalopram, escitalopram, fluvoxamine
Indications: MDD, GAD, OCD, PTSD, panic disorder, premature ejaculation, binge eating disorder, bulimia nervosa, SAD, gambling disorder
Side effects: Headache, N+V, diarrhea, agitation, anxiety (these should resolve within 1 week). Sexual dysfunction; serotonin syndrome - tremor, nausea; SIADH.
Meloxicam (mobic, moxicam, melobic)
Selective COX-2 inhibitor NSAID
NSAIDS - MOA, agents, side effects, contraindications
MOA: Analgesic, antipyretic and anti-inflammatory actions. Inhibit synthesis of prostaglandins by inhibiting cyclo-oxygenase (COX) present as COX1 and COX2
- Inhibition of COX1 results in impaired gastric cytoprotection and antiplatelet effect
- inhibition of COX2 results in anti-inflammatory and analgesic action
- Reduction in GFR and renal blood flow occurs with both COX1 and COX2 inhibition
Most NSAIDs are nonselective, inhibiting both COX1 and COX2. Reversible inhibition of COX1 and COX 2 causes decreased prostaglandin synthesis. Aspirin irreversible.
Agents: Ibuprofen, diclofenac, indomethacin, naproxen, meloxicam, piroxicam, ketorolac, aspirin
Side effects: Gastric and duodenal ulcers, increased risk of heart attack and stroke (not with aspirin and naproxen), renal function impairment (prostaglandins maintain renal blood flow by vasodilating afferent arterioles)
Contraindications: Acute haemmorhage, gastroduodenal ulcers, renal failure, pregnancy, pre-surgery (cease 1-3 days prior)
Selective COX-2 inhibitor NSAIDs - MOA, agents, indications, side effects, contraindications
MOA: selectively inhibit COX-2 enzyme with no or minimal inhibition of COX-1. (COX-2 found in cells that mediate pain and inflammation - macrophages, leukocytes; and vascular endothelial cells)
Analgesic and anti-inflammatory, advantageous over non-selective due to no anti-platelet effect, minimal gastric side effects and reduced risk of gastric ulcers
Agents: Celecoxib
Indications: RA, OA, acute pain, patients with history of peptic ulcer disease and platelet disorders
Side effects: increased risk of thrombosis, MI, stroke; sulfa drug reaction
Contraindications: Severe HF, recent MI or GI bleed, sulfa drug allergy
Indometacin
nonselective NSAID
Diclofenac
Nonselective NSAID
Xanthine oxidase inhibitors - MOA, agents, indication, side effects
MOA: Inhibit xanthine oxidase which reduces production of uric acid, lowering serum urate concentration and allowing acute flares and crystal deposits to resolve if long-term serum urate <0.36mmol/L
Agents: Allopurinol (preferred first line treatment), febuxostat
Indication: Urate-lowering therapy, gout
Side effects: Rash, stevens-Johnson syndrome/toxic epidermal necrolysis
Allopurinol: class + indications
Xanthine oxidase inhibitor
Indications: symtomatic hyperuricemia (gout)
Febuxostat (class + indications)
Xanthine oxidase inhibitor
Indications: symtomatic hyperuricemia (gout) - second line behind allopurinol
Cefalexin (cephalex, ibilex, keflex, cephalexin) - class and indications
Cephalosporin
Staphylococcal and streptococcal infections in people with mild to moderate penicillin allergy, UTI, epididymo-orchitis (urinary tract source)
Cefazolin - class
Cephalosporin (Abx)
Cefaclor - class
Cephalosporin (Abx)
Cephalosporins - MOA, agents, coverage, indications, side effects
MOA: Broad-spectrum. Interfere with bacterial cell wall peptidoglycan synthesis by binding to penicillin-binding proteins, eventually leading to cell lysis and death; bactericidal.
Agents:
1st generation: Cephalexin (oral), cefazolin (IV, IM)
2nd generation: Cefaclor, cefuroxime (oral)
Coverage: Highly active against gram +ve bacteria, 1st - 3rd gen most to least active. Active against some gram -ve bacteria (proteus mirabalis, e coli, klebsiella pneumoniae, no atypical coverage (chlamydia, mycoplasma, legionella). Indications: Cefazolin for perioperative wound infection prophylaxis (covers s. aureus). Ceftriaxone specifically has good CNS penetrance - meningitis, also used for gonnorhea and lyme disease
Side effects: Vitamin K deficiency, autoimmune hemolytic anemia
Carbapenems - MOA, agents, coverage, indications, side effects
MOA: Inhibit bacterial cell wall synthesis by binding to penicillin-binding proteins, the affinities for which differ between the carbapenems and may affect their activity in vitro; usually bactericidal.
Agents: Imipenem, meropenem, ertapenem, doripenem (all IV)
Coverage: Broad spectrum w intrinsic beta lactamase resistance; gram positive cocci (except for MRSA, enterococcus fecalis and enterococcus faecium) gram -ve rods, anaerobes
Indications: Last resort drugs (used in life threatening infections or after other antibiotics due to significant adverse effects)
Side effects: Secondary fungal infections, CNS toxicity - can lower seizure threshold at high serum concentrations, GI upset, rash, thrombophlebitis
Macrolides - MOA, agents, coverage, indications, side effects, special considerations, contraindications
MOA: Bacteriostatic; inhibit bacterial protein synthesis by binding to the 23S ribosomal RNA molecule of the 50S ribosomal subunit leading to inhibition of bacterial protein synthesis. They also have immunomodulatory and anti-inflammatory effects.
Agents: Erythromycin, azithromycin, clarithromycin (oral or IV), roxithromycin (oral).
Coverage: Atypical pneumonia caused by mycoplasma pneumonia, legionella pneumonia, chlamydophilia pneumoniae; bordetella pertussis, chlamydia, gram +ve cocci (esp streptococcal infection in pts allergic to penicillin), neisseria (dual therapy with ceftrizxone for N. gonorrhea - azithromycin, mycobacterium avium, h pylori
Side effects: GI upset (increased intestinal motility), QT interval prolongation (arrhythmia), eosinophillia, rash, increased risk of hypertrophic pyloric stenosis (erythromycin and azithromycin) in infants up to 6 weeks of age
Special considerations:
Poor CNS penetration, biliary elimination, short half life
CI’s: Pregnancy (erythromycin and clarithromycin (teratogenic), hepatic failure, children <12, renal failure
Azithromycin
Macrolide
Clarithromycin
Macrolide
Erythromycin
Macrolide
Natural penicillin - MOA, agents, coverage, indications, side effects
MOA: Bactericidal; interfere with bacterial cell wall peptidoglycan synthesis by binding to penicillin-binding proteins, eventually leading to cell lysis and death.
Agents: Natural: Penicillin G (benzylpenicillin) - IV (crystalline penicillin G), IM (procaine penicillin G, benzathine penicillin G)
; penicillin V (phenoxymethylpenicillin) - oral.
Coverage: Gram +ve aerobes (esp streptococcus pyogenes, strep pneumoniae). Gram -ve cocci (esp neisseria meningitidis). Spirochetes (esp. treponema pallidum). Branching gram +ve anaerobes (esp actinomyces)
Side effects: Hypersensitivity reactions, hemolytic anemia positive direct coombs test, drug induced interstitial nephritis, seizures
Amoxicillin - class and indications
Penicillin
Indications - exacerbation of chronic bronchitis, CAP, acute otitis media, sinusitis, gonococcal infection, epididymo-orchitis, acute prostatitis, acute pyelonephritis, UTI, endocarditis prophylaxis in high risk patients, acute cholecystitis, peritonitis, eradication of H pylori
Amoxicillin with clavulanic acid (amoxiclav) MOA
Clavulanic acid inhibits beta-lactamase, which extends spectrum of activity of amoxicillin with clavulanic acid to cover some beta-lactamase-producing organisms.