Things to remember

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Things to remember
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2011-10-04 09:35:27
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Things to remember about particular drugs/drug classes
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  1. Systemic photosensitisers
    • amiodarone
    • griseofulvin
    • NSAIDs
    • phenothiazines (chlorpromazine, pimozide, clozapine, promethazine, etc. - 'z-drugs')
    • methoxsalen (for psoriasis)
    • quinolones (ciprofloxacin, moxifloxacin, norfloxacin, ofloxacin)
    • retinoids (acitretin, adapalene, isotretinoin, tazarotene, tretinoin)
    • SJW
    • tetracyclines (doxycycline, minocycline, tetracycline) thiazides (rare)
  2. Topical sensitisers
    • triclosan
    • coal tar derivatives
    • fragrances
    • methoxsalen
    • retinoids (adalaplene, isotretinoin, tazarotene, tretinoin)
    • sulfonamides
  3. sulphonylureas preferred in elderly
    gliclazide and glipizide
  4. Thiazolidinediones - ADRs
    • wt gain
    • anaemia
    • oedema
    • heart failure
    • CV ischaemic events (possibly)
    • C/I with insulin - inc risk of HF
    • C/I - T1DM, ketoacidosis, Insulin tx, HF (except pioglitazone in class 1)
    • Rosiglitazone - increases in HDL and LDL cholesterol
    • Pioglitazone - myalgia
  5. Insulin - counselling pts
    • EtOH - decreases blood glucose, may mask warning signs of hypos, avoid binging, eat something when you drink
    • friends and family to know sx and tx of hypos
    • inject s/c into abdomen OR thigh/upper arm/buttock
    • SA - 30 mins before meals
    • ultra-short acting - immediately before meals
    • resuspend cloudy insulin (long-acting - humulin, isophane, protaphane) gently rotate vials/cartridges of cloudy insulin
    • sulphonylureas - often stopped/reduced once tx est'd, metformin/pioglitazone may be continued - rosiglitazone C/I
  6. Sitagliptin - class
    • DPP-4 inhibitor
    • MOA: inc conc of incretin hormones (e.g. GLP-1) - increases G-dependent I secretion, reduces glucagon production
    • Precaution - tx with ACE-i - inc risk of angiodema
    • Sfx: hypos, infections, headaches, constipation (infreq)
  7. Acarbose
    • Swallow whole before meals or chew with first mouthfuls of food
    • give glucose but not sucrose (cane sugar) for hypos
    • flatulence, diarrhoea, abdominal pain and distension common ADRs
  8. Exanitide
    • GLP-1 analogue: up insulin, down glucagon (enhances glucose-dependent insulin secretion and suppresses inappropriate glucagon secretion), delays gastric emptying = reduced G absorption rate and decreases appetite
    • inject 60 mins before main meals at least 6 hrs apart - BD dosing
    • slow stomach emptying - may affect other meds, ensure ABx given at least 1 hr before/4 hrs after exanitide
  9. Thyroxine - PPs
    • empty stomach, pref before breakfast
    • tell if sx of hyperthyroidism occur - palpitations, excitability, insomnia, flushing, sweating, weight loss
  10. bisphosphonates - MOA
    inhibit osteoclasts (decrease bone resorption)
  11. bisphosphonates - ADRs
    • common: n, v, d, headache, hypocalcaemia, muscoloskeletal pain
    • rare: osteonecrosis of the jaw (risk higher w/ infusion)
    • concomitant use of NSAIDs increases irisk of oesophageal adverse effects
  12. cholecalciferol vs. calcitriol
    • cholecalciferol - slow onset (4-8 weeks), long duration of action (8-16 weeks)
    • calcitriol - rapid onset (1-3 days), short duration of action (<1 week), active, higher risk of hypercalcaemia
  13. Raloxifene
    • SERM
    • oestrogen agonist effects on bone
    • antagonistic effects on other oestrogen-receptive tissue, e.g. breast and endometrium
    • prevention and tx of post-menopausal OP, Primary prevention of BREAST CANCER in high-risk post-menopausal women
    • Precautions: VTE hx/risk, CAD
    • C/I in pregnancy - cat X
    • common ADR: hot flushes (may also aggravate), sweating, leg cramps, p oedema, sleep disorders
    • ensure adequate intake of Ca and Vit D
  14. corticosteroid replacement therapy in adrenal insufficiency - PPs
    • give in 2 doses - 2/3 mane, 1/3 evening
    • usual contraindications do not apply
    • increase in therapy required during illness and stress --> mild infection = 2-3X dose, serious infection/sx --< IV
  15. eye drops - practice points
    • write date you open - 28/7
    • wash your hands, then sit or lie down
    • tilt head back and look up and gently pull down lower lid to create pouch
    • 1 dop into pouch - close eyes and gently press against inner corner of eye (over tear duct) for at least 3 mins
    • avoid letting top of dropper touch your eyes, skin or other surface
    • another drop - allow 5 mins
    • clean tissue to mop up excess
    • get someone to help/mirror/eye dropper
    • try storing in fridge - know when drop in eye
    • contact lenses - wait at least 15 mins after before inserting
  16. eye ointments
    • squeeze small amount (1cm) along pouch then blink several times to spread the ointment
    • if using drops, use oinment last
  17. eye infections - PPs
    • clear away debris and mucus with NS before using medication if possible
    • no improvement in 2 days - refer/r/v diagnosis
    • contact lenses should not be worn for 24 hrs after infection resolved
  18. viral conjunctivitis - tx
    • regular use of artificial tears
    • cool compresses
    • hygeine - avoid sharing facial towels, touching face, etc
    • infection until redness and weeping resolves - no antivirals
  19. blepharitis
    • Seborrhoeic dermatitis of lid margin - greasy, easily removed scales on lid margin
    • warm compress (face cloth in warm water - apply for 5-10 mins BD)
    • scrub lids BD - 1:10 baby soap:water
  20. glaucoma eye drops - lines of tx
    • 1: PG analogues
    • 2: BBs
    • 3: CA-i's
  21. drug classes for open angle glaucoma - doses/day
    • BBs (e.g. timolol) --> D-BD
    • PG analogues (e.g. latanoprost) --> D (nocte)
    • Carbonic Anhydrase-i's (dorzolamide) --> BD-TDS
    • A2 agonist (e.g. brimonidine) --> BD-TDS
  22. BB eye drops - PPs
    • use generally C/I in CAL - betaxolol cardioselective and preferred
    • consider systemic effects - C/I in bradyarrhythmia, AV block
    • oral BBs lower IOP - consider alternate class as may be more effective and lower risk of adverse fx
    • avoid tx with verapamil --> profound bradycardia
    • ADR: stinging on instillation, bradycardia
    • timolol - non-selective, fewer local fx
    • betaxolol - selective for B1, stinging
  23. PG analogues - PPs
    • evening for optimal effect
    • structurally different - consider another drug in this class if response to one is poor
    • paradoxical increase in pressure if 2 PG analogues used together - avoid combination
  24. Carbonic anhydrase inhibitors - PPs
    • allergy to sulphonamides - risk of allergy
    • common ADR: occular irritation, foreign body sensation bitter taste
    • avoid driving if you exp blurred vision
  25. treatment for allergic conjunctivitis - mild sx:
    • NS BD
    • artificial teas - 4-8 times daily
    • cold water compresses as required
  26. tx for allergic conjunctivitis - moderate sx
    • topical drugs:
    • ketorolac (acular) - 2-4 wks only - 1 QID
    • levocabastine (livostin) - 1 BD
    • ketotifen (zaditen) - 1 BD
    • olopatadine (patanol) - 1 BD
    • azelastine (Eyezep) - 1 BD
    • recurrent disease - cromoglycate
  27. antihistamine eye drops
    • azelasatine (eyezep)
    • levocabastine (livostin) - may cause drowsiness
    • ketotifen
    • olopatadine
    • ketotifen (zaditen) and olopatadine (patanol) also have mast-cell stabilising effects
  28. Cromoglycate (Opticrom) - PPs
    • mast cell stabiliser
    • may take 3-6 weeks to reach full effect - i.e. delayed onset of action, 2-4 weeks for noticeable effect
    • start tx 1 month before hayfever season or use oral/topical antihistamines until it takes effect
  29. secondary causes of dry eyes - drugs
    • anticholinergics
    • diuretics
    • OCP
  30. Dry eye drops - drug choice
    • preservative containing:
    • infrequent use - inexpensive product
    • frequent use - product with less irritant preservative, e.g. polytears, genteal
    • preservative free:
    • non-irritant, but more expensive (bulky single dose)
    • useful for use >4-6/day, contact lens wearers, allergy to preservative
    • single vials can be used more than once, but discarded in 24 hrs
    • ointments/gels: use at bedtime
  31. Dose equivalence of PPIs
    pantop 40mg = omeprazole/esomeprazole/rabeprazole 20mg = lansoprazole 30mg
  32. N+V tx in pregnancy
    • most common during first trimester
    • ensure ADEQUATE HYDRATION
    • ginger (up to 1g D) or pyridoxine (vitamin B6 - 25-50mg TDS PRN)
    • if these are ineffective, consider: doxylamine, metoclopramide, promethazine or prochlorperazine
    • prochlorperazine suppositories if n+v severe
  33. dopamine agonists in n+v - PPs
    • domperidone, droperidol, haloperidol, metoclopramide, prochlorperazine
    • EPSE (usually acute dystonic reactions*) due to central dopaminergic activity may occur - more common in elderly and <20yrs
    • EPSE rare with domperidone - does not X BBB*mainly muscle spasms of face, neck, back and limbs
    • domperidone and metoclopramide - widely used, additional prokinetic activity (good for n/v due to gastroparesis)
    • prochlorperazine - PREVENT n+v
    • droperidol - PONV
  34. constipation - dietary and lifestyle changes
    • drink water - enough to satisfy thirst and keep urine light-coloured (unless restricted by Dr)
    • exercise - develop abdominal muscles
    • increase fibre intake - grains, fruits, vegetables; 25-30g D recommended in adults, increase intake gradually to avoid bloating
    • use toilet after meals - gastrocolic relfex maximal - 'gut is most active'
    • do no resist urge to go
  35. laxatives - class and time to effect
    • bulking agents: 2-3 days
    • osmotic laxatives:
    • glycerol, lactulose, sorbitol - oral 1-3 days, rectal: 5-30 mins;
    • polyethylene glycol (Glycoprep, movicol)- oral - 0.5-3 hrs for bowel preparation, 1-4 days for constipation
    • saline laxatives (epsom salts, microlax, fleet, picolax, picoprep)
    • stool softeners: oral - 1-3 days, rectal: 5-20 mins
    • stimulant laxatives: oral - 6-12 hrs, rectal - 5-60 mins
  36. constipation in pregnancy
    • dietary and lifestyle changes preferred
    • bulking agents to supplement fibre intake
    • docusate, lactulose, sorbitol safe
    • occasional doses polyethylene glycol (e.g. movicol) ok if resistant to the above
    • stimulant laxatives - avoid
  37. diarrhoea in children
    • 1: ORS
    • antidiarrhoeals not recommended - do not reduce fluid and electrolyte loss, may delay expulsion of organisms, may cause ADRs
  38. tx of diverticular disease
    • --> diarrhoea
    • 1: bulking agents usu useful
    • if diarrhoea persists - add opiod antidiarrhoeal, e.g. loperamide
  39. Traveller's diarrhoea - tx
    • 1: norfloxacin
    • 2: azithromycin (suitable in pregnancy and children)

    • advise on avoiding/treating infection
    • treat symptomatically if mild - ORS - tx for 1-3 days
    • seek medical advice if, e.g. bloody diarrhoea, fever
    • loperamide may be useful in adults
  40. Giardiasis-induced diarrhoea - tx
    • 1: tinidazole - as a single 2g (4 X 500mg) dose, give as divided doses in pregnancy
    • 2: metronidazole - for 3-7 days, use in children
    • adult - 2g once D for 3 days, or 400mg TDS for 7 days if tx fails, children, pregnancy and breastfeeding
    • do not tx asymptomatic carriers unless they handle food
    • take with food
  41. Treatment for Crohn's - drug choice
    • depends on goal - remission or induction + other factors:
    • 5-aminosalicylates - induce remission in mild-mod disease
    • corticosteroids - induce remission (usu 7-14 days), then wean
    • Azathioprine + mercaptopurine - induce and MAINTAIN remission, have corticosteroid sparing effect, onset may be up to 3 MONTHS - use adjuvant in interim, no direct comparisons - if not responsive to one, try the other
    • MTX - induce remission, prevent relapse - mainly used in pts refractory to/intolerant of AZA and mercaptopurine
    • TNF-A antagonists (infliximab, adalidumab) - unresponsive mod-severe disease
    • antibacterials (metronidazole/ciprofloxacin) - for perianal fistulae
    • other: antidiarrhoeals, cholestyramine (+ im B12) = may reduce diarrhoea
  42. Ulcerative colitis - drug choice
    • 5-ASAs - induce and MAINTAIN remission in mild-mod disease, combination of rectal and oral synergistic; for distal colitis - choose rectal mesalazine
    • corticosteroids - induce remission in severe/refractory acute disease (7-14/7)
    • azatioprine + mercaptopurine - limited ev in UC, used for maintaining remission and corticosteroid-sparing effects, onset may be 3/12
    • cyclosporin: iv, rapid onset (usu 1 week) for severe, unresponse disease, once in remission, use other agents for maintenance
    • Infliximab - induce and MAINTAIN remission in unresponsive, mod-sev disease
    • antidiarrhoeals (eg. loperamide, codeine) - CONTRAINDICATED (risk of toxic megacolon)
    • Antispasmodics - not recommended
  43. lifestyle advice for BPH
    • look for aggravating factors - constipation, diuretics, anticholinergics, sedating drugs
    • reduce caffeine and EtOH intake
    • bladder training
    • reduce fluid intake at night
  44. BPH - drug choice
    • selective A-blockers - 48 hrs to effect
    • 5-A- reductase inhibitors - reduce prostate size, may take 6 months before sx improve (12-18 months for full effect)
    • both inc urinary flow rate
    • combination - when prostate large and rapid relief required, selective alpha blocker can be stopped at 6-12 months in mst pts
  45. antibiotic to avoid in prostatitis
    nitrofurantoin - penetrates prostatic tissue poorly
  46. OA - lines of therapy
    • 1: lifestyle (regular exercise + other - wt loss, physical activity, devices - walking stick)
    • 1: regular paracetamol
    • 2: topical NSAID, capsaicin, rubefacient + reg paracetamol
    • 3: PRN NSAID (e.g. 30-60 mins b4 painful activity), intra-articular steroids, hyalans
    • 4: higher NSAID dose
    • 5: opiods, orthopaedic r/v
    • NB: many pts on LT NSAIDs can be switched to paracetamol w/out inc in sx
  47. NSAIDs - MOA
    • analgesic, antipyretic, anti-inflammatory
    • inhibit PG synthesis via COX-inhibition
    • - COX-1 inhibition = impaired gastric cytoprotection and antiplatelet effects
    • - COX-2 inhibition = anti-inflammatory and analgesic activity
    • - reduction in GFR and renal blood flow occurs through both COX-1 and COX-2 inhibition
    • little-no effect on COX-1 inhibitors at therapeutic doses of COX-2-i's
  48. NSAIDs - PPs
    • no rationale for >1
    • maximal effect in 2 weeks. no response = switch after 3 weeks
    • monitor FBC, Cr, LFTs
    • lowest effective dose for shortest possible time
  49. RA - PPs
    • ensure all pts receieve pneumococcal and annual influenza vaccinations
    • withdrawal in apparent remission --> relapse
  50. RA - lines of tx
    • disease suppression: antirheumatic agent + analgesic, corticosteroid (low dose pred) or NSAID
    • mild-disease activity: sulfasalazine or hydroxychloroquine (sulfasalazine acts sooner and more effective)
    • mod-severe disease: low-dose MTX (1st line), other immunosuppresants; leflunomide or cytokine modulators (biological agents, e.g. rituximab) when antirheumatics/immunosuppresants (inc MTX) inappropriate/ineffective
    • combination often needed to slow progression of jt damage (e.g. rituximab + MTX)
  51. malaria prevention
    • use insect repellants
    • wear protective clothing
    • take medications regularly/at right time
    • See Dr if fever develops w/in 12 months of possible exposure
  52. Gout - tx during anticoagulation
    • 1: systemic corticosteroids
    • 2: colchicine
    • avoid NSAIDS - risk of bleeding
  53. acute soft tissue injuries - tx
    • bursitis/tendonitis:
    • rest injury - by avoiding painful activities, not immobilisation
    • passive motion exercises
    • local heat/ice packs
    • analgesics - reduce pain, aid mobilisation - paracetamaol and NSAIDs have similar efficacy
    • also consider topical NSAIDs and rubefacients
    • strains + sprains:
    • RICE for first 2 days
    • early mobilisation and recovery - use analgesics
    • topical NSAIDs or rubefacients
  54. Paracetamol + back pain
    no evidence for its efficacy in this condition
  55. rubefacients and other topical musculoskeletal agents
    • apply BD - QID PRN for up to 14 days, r/v use after this
    • rub product in completely as may stain clothing and temporarily discolour skin
    • photosensitivity
  56. seizure precipitants
    • lack of sleep
    • stress
    • alcohol withdrawal
    • ilicit drugs
    • changes in medication/non-compliance
  57. antiepileptics which induce CYP3A4s
    CBZ, PHY, oxCBZ, barbiturates, topiramate

    reduce efficacy of oral contraceptives - consider medroxyprogetserone depot or copper IUD if possible, or high-dose COC if not.
  58. CBZ - PPs
    • TDM - th range = 4--12mg/L
    • take with food
    • drowsiness and blurred vision at start of tx
    • increase fx of EtOH
    • CYP3A4 inducer
    • refer if: rash, sore throat, fever, mouth ulcers, bruising, bleeding
    • do not stop taking suddenly
    • increase dose slowly - autoinduction
    • monitor for skin reactions - SJS, toxic epidermal necrolysis
    • BMD monitoring - vit D + cal if needed
  59. Anticholinergics
    • atropine
    • belladona alkaloids (atropine, hyoscine)
    • benzhexol
    • benztropine
    • darifenacin
    • glycopyrrolate
    • hyoscine
    • iptratropium
    • oxybutynin
    • solifenacin
    • tiotropium
    • tropicamide
  60. Migraine - lines of tx
    • 1: simple analgesic - paracetamol (less effective), aspirin, NSAID
    • 2: if ineffective (e.g. for 3 attacks/severe): triptan, ergot alkaloid at onset of attack
    • antiemetic for n+v (metoclopramide/domperidone)
    • avoid opiods - may aggravate sx, dependence, little evidence
  61. Triptans - PPs
    • 5HT1 agonists
    • relief w/in 30-60 mins (longer with naratriptan)
    • aid associated sx (n, v, photophobia, phonophobia)
    • 1/3 may have recurrence of headache - give 2nd dose
    • most effective when taken when headached BEGINNING TO DEVELOP, not earlier (during aura) or later (when headache severe)
    • sumatripatn most studied
  62. ergot alkaloids - PPs
    • limited by ADRs - peripheral vasoconstriction
    • taken at onset of attack
    • do NOT take with triptan
    • lack of ev re dose
    • rectal/sc/im
  63. Drugs in migraine prevention
    • 1: BBs (propranolol, metoprolol, atenolol), amitriptyline
    • 2: valproate, topiramate
    • 3: methysergide, pizotifen - but limited by ADRs

    treatment of acute attacks still needed - may take 1-3 months for full effect
  64. Secondary prevention of stroke
    • antiplatelet - asprin, clopidogrel, dipyridamole with aspirin (headache + BD dosing affect compliance, but more effect than aspirin alone)
    • warfarin in AF
    • antihypertensives
    • statins
    • carotid sx (high risk pts)
  65. SSRIs - PPs
    • - most ppl can be maintained w/ 10mg escitalopram, 20mg citalopram, paroxetine, fluoxetine, 50mg sertraline, 50-100mg fluvoxamine
    • - doses may be higher in the tx of OCD and eating disorders (vs. if for depression or anxiety)
    • - withdraw gradually - 50% weekly
    • - fluoxetine has an active metabolite and long half life = long wash over
    • - lower seizure threshold
    • - increase bleeding risk - consider PPI
    • indications: depression, OCD. PTSD, PMS
  66. TCAs - ADRs
    • sedation
    • anticholinergic
    • orthostatic hypotension
  67. Precautions of antipsychotics
    • PD - risk of aggravation
    • epilepsy - lowers seizure threshold
    • respiratory failure - resp dep
    • hyperthyroidism - risk of acute dystonia
    • QT prolongation
    • shock - hypotension
    • glaucoma, urinary retention - anticholinergic fx (esp chlorpromazine, clozapine, olanzapine)
    • elderly - higher risk of orthostatic hypotension, confusion, anticholinergic fx, acute EPSE
    • ADRs traditionally reported with older agents, less common/severe with newer ones
  68. common sfx of antipsychotics
    • sedation, EPSE*, orthostatic hypotension, blurred vision, constipation, anticholinergic fx, wt gain, hyperprolactinaemia (--> womanising fx)
    • metabolic fx: inc BSL, wt gain, dyslipidaemia, inc risk of T2DM
    • EPSE - dystonia (spasms) - have benztropine on hand, akathisia (feeling of motor restlessness), parkinsonism (tremor, rigidity, bradycardia - tardive), tardive dyskinesea (involuntary movements after M-LT tx)
  69. comparison of sfx of conventional antipsychotics - sedation, anticholinergic, EPSE, othostatic hypotension, metabolic
    low potency - more sedating, low EPSE, more othostatic and anticholinergic fx

    • low potency = chlorpromazine
    • high potency = haloperidol

    atypical APs generally have lower incidence of EPSE
  70. Bipolar - mood stabilisers - monitor
    electrolytes, LFTs, blood picture
  71. ADHD - drug choice
    • 1: psychostimulants - dexamphetamine, methylphenidate (give more than once d, except low doses or CR methylphenidate)
    • 2: atamoxetine (risk of suicidal thoughts/beh)
    • 3: TCAs, clinidine (A-adrenergic, sedative properties)
    • SSRIs not indicated
  72. adverse effects of nicotine
    • alters HR
    • constricts coronary blood vessels - IHD + thromboembolism
    • benefis of stopping smoking: red MI risk and premature death
  73. advice on quitting smoking
    • behavioural techniques to aid and encourage cessation (e.g. avoiding triggers)
    • refer to quitline (13 QUIT)
    • nutritional advice (e.g. fruit for snacks)
    • exercise program - help avoid wt gain
    • NB: withdrawal effect = hunger
  74. Smoking cessation - drug choice
    • bupropion (Zyban) - X2 quit rate; inhibits NA and dopamine uptake - prec with schizo and dep; insomnia (40%) and seizures
    • NRT - X2 quit rate
    • varenicline (Champix) - >2X quit rate; partial agonist at nicotine Rs, reduces withdrawal and pleasurable effects of smoking; nausea (30%) - may req dose red, apparent withdrawal and return to smoking on tx cessation
  75. Precautions with theophyllines
    • GORD - inc gastric acid
    • arrhythmia - exacerbation
    • HF, pulmonary oedema - red clearance = red dose
    • thyroid dysfn - hyperT = inc CL, hypoT = dec CL - adjust dose
    • smoking - inc CL
    • epilepsy - dec seizure threshold
    • B2 ag = inc risk hypoK
    • TOXICITY: common - GORD, insomnia, palpitations; rare - seizures

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