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Top drug profile (Summary)

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Pharmacy

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University Of East Anglia

It is a summary of medications, including indications, mode of action, contraindications, common side effect, point of interest/ counselling points, interactions. More than 100 commonly used medications It is suitable for revision for MPharm examinations and GPHC pre-registration examinations N...

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pharmacology
pharmacy
top drug profile
medications profile
medications

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Billy’s Top drugs profiles & pharmacology

Opioid analgesics
MOA: mu-opioid agonist that can bind to glutamatergic NMDA receptor, thus acting as a receptor antagonist against glutamate
Classifications of opioid analgesics:
 Strong opioid: morphine (drug of choice for PO severe pain in palliative care), buprenorphine, dipipanone, diamorphine, alfentanil, fentanyl, remifentanil, methadone, papaveretum, pentazocine (partial
agonist), pethidine (very short action), tapentadol, tramadol
 Weak opioid: codeine, dihydrocodeine, meptazinol
General information about opioids:
 Dose adjustment:
1) Increment of morphine should not exceed 1/3 to ½ of the total daily dose every 24 hours
2) Breakthrough pain (given 30 minutes before activity that causes pain): 1/10-1/6 of the regular 24-hour dose (given q2-4h, up to hourly if severe/last days of life)  morphine sulphate
10mg/5ml or oxycodone (immediate-release) can be used in breakthrough pain
 CCI: acute resp depression, head injuries/ raised intracranial pressure (opioid analgesic can interfere with pupillary response vital for neurological assessment), comatose pt, risk of paralytic ileus
 Caution: reduce dose in adrenocortical insufficiency/ elderly/ hypothyroidism, asthma (avoid during attack), convulsion, biliary tract disease, hypotension, IBD, MG, prostatic hypertrophy
 S/E (long term use):
o dose-related hypogonadism and adrenal insufficiency  amenorrhoea, reduced libido, infertility, depression, erectile dysfunction
o hyperalgesia (reduce dose of opioid/ switch therapy)
o resp depression (treated by artificial ventilation/ reversed by naloxone)
o overdose: cause symptoms e.g. coma, resp depression, pinpoint pupil, constipation, loss of appetite, reduced consciousness, n/v (antidote: naloxone)
 P: CCI due to resp depression, withdrawal symptoms in neonates (when used during delivery); gastric stasis, aspiration pneumonia in mother (when used during labour)
 Hepatic: avoid/ reduce dose (may precipitate coma)
Generic name Indications (other CCI (other CCIs in bold) CSE (other S/E) MOA/POI/ BP/ renal & hepatic impairment (other information in bold)
– drug class indications in bold)
Codeine  mild to moderate pain  obstructive airway disease n/v,  [4] (1) tablet should not be crushed (2) overdose can cause hyperalgesia (3) avoid abrupt
phosphate  short term treatment of  acute respiratory depression drowsiness, withdrawal (4) don’t drive
– MOR acute moderate pain  head injuries that increase dependence, dry  B: avoid (may present in milk and cause opioid overdose in fetus)
agonist  acute diarrhea intracranial pressure mouth,  Renal: avoid/ reduce dose (increase cerebral sensitivity)
 dry cough  risk of paralytic ileus constipation  Use of codeine in children: not indicated for < 12 (max dose for 12-18 = 240mg/d, use lowest
 acute ulcerative/ antibiotics- effective dose, max 3/7 use)
associated colitis  Prevalence of CYP2D6 metabolizer: North American/ Ethiopian/ Arabs > Caucasian > African
 patients at all ages with known American > Hispanics/ Chinese/ ulphur
ultra-fast codeine metabolizer  PK: metabolized in liver by 2D6 to morphine via O-demethylation; excerted via urine (main) &
(CYP2D6) faeces (metabolized mainly in liver by CYP – not suitable in liver failure – can use dihydrocodeine
 <18 with tonsils/ adenoids 15mg as single dose and monitor effects)
removal for treatment of sleep
apnoea
Diamorphine  acute pain  delayed gastric emptying taste disturbance,  Renal: avoid/ reduce dose
– MOR  MI (acute treatment)  phaeochromocytoma (medulla anorexia,  mixing and compatibility:
agonist  acute pulmonary oedema tumor that secrete high amount of increased o Diamorphine SC max 250mg/ml (max 40mg/ml + water for injection/ normal saline)
catecholamine) intracranial o cyclizine (>10mg/ml) or in the presence of normal saline may precipitate after 24 hrs
pressure o haloperidol (>2mg/ml) + diamorphine may precipitate after 24 hrs
 Caution: CNS depression, severe diarrhea, severe cor pulmonale (pulmonary heart disease),
toxic psychosis
Morphine –  acute/ severe pain  impaired respiratory function n/v, constipation,  [4] (1) tablet should not be crushed (2) may cause dependence (3) liable to addiction (4); monitor
MOR agonist  chronic pain  head injuries dependence, pain relief and S/E
 acute pulmonary  renal and hepatic impairment drowsiness  Renal: avoid (reduce dose)
oedema  delayed gastric emptying  PK: metabolized in liver and gut via glucuronidation to produce morphine-3-glucoronide and
 dyspnea in palliative  phaeochromocytoma morphine-6-glucoronide; undergoes extensive first-pass metabolism; excreted mainly via urine/
care minor via faeces
 PCA  Oral solution: contain ethanol as excipient (may interact with metronidazole/ not suitable liver
 cough in terminal failure, alcoholism) (discard 3/12 after opening)
illness
Methadone–  severe pain  impaired respiratory function n/v, constipation,  [3] (1) don’t drive (2) enhanced effect with alcohol (3) avoid in renal and hepatic impairment
MOR agonist  cough in terminal illness  head injuries drowsiness,  B: OK during maintenance therapy (monitor S/E in infants)
 adjunct in the treatment  comatose state headache,  Caution: QT prolongation/ taking other medications that can cause QT prolongation
of opioid dependence  phaeochromocytoma hallucination

,Buprenorphin  moderate to severe pain  impaired respiratory function DDGSBTHH  [4] (1) caution in: dependence, hypotension, when starting/ ending patches before/ after other
e  adjunct in the treatment  head injuries dry mouth, opiates (2) enhanced effect with alcohol (3) long duration of action compared to morphine
– Partial of opioid dependence  paralytic ileus drowsiness, GID, (4) effect only partially reversed by naloxone
agonist of sweating,  B: Low level present in breast milk
MOR & KOR bradycardia,  Renal + hepatic: avoid
tachycardia,  Specific caution: (transdermal patch) other opiates should not be given within 24 hrs of patch
hypotension, removal in adult due to long DOA; (when used in adjunct in opioid dependence); hepatitis B, C
headache infection, pre-existing enzyme abnormality; (interactions) concomitant use with hepatotoxic drugs;
(fever) may increase absorption
 Partial agonist  may precipitate withdrawal symptoms
 PK: hepatic metabolism via oxidation by CYP3A4 isoenzyme to the pharmacologically active
metabolite N-dealkylbuprenorphine (norbuprenorphine); excreted via faeces mainly
Fentanyl –  severe pain  risk of paralytic ileus dry mouth,  [6] (1) patch changed every 72 hrs (2) caution in: renal and hepatic impairment, hypotension,
MOR agonist  post op analgesic dizziness, dependence, impaired resp function (3) monitor increased S/E (4) care when starting/ ending
 breakthrough pain headache, GID, patches (5) increased risk of resp depression in opioid naïve patient (6) don’t drive
urinary retention,  B: OK (monitor S/E in infants)
Dose conversion of 24 hrly PO morphine dose to 72hrly
insomnia, HT,  Renal: avoid/ reduce dose (alfentanil preferred in renal disease due to very short elimination
fentanyl patch:
tremor, vaso- half-life and it is hepatically metabolized)
dilation,  Specific caution: mucositis (increased PO absorption)
Morphine salt daily (mg) Fentanyl patch (mcg/hr) anorexia,  PK: metabolized in liver via N-dealkylation and hydroxylation by 3A4 isoenzyme; excreted via urine
30 12 myoclonic (main)/ faeces (minor)
60 25 movement (IV)  Instructions of using the patch:
90 37.5 1. clean the skin with cold water (don’t use soap, oil & do not stick the patch on straight after a
120 50 hot bath or shower)
180 75 2. it is waterproof (don’t scrub the patch)  can bath, shower, swim
240 100 3. do not expose patch in direct heat (e.g. hot water, sunbath)  may increase the amount of
medicine entering the systemic circulations
4. apply on the upper body/ arms (no joints) in adult and upper back in children
5. stick a new patch straight away if the old one falls off (then record the time  change after 3
days)
Oxycodone –  Severe pain  Acute abdomen  Renal: avoid eGFR<10 (max 2.5mg Q6H with mild to moderate renal impairment)
MOR agonist  PCA  Chronic constipation
 Moderate/ severe pain  Delayed gastric emptying
in palliative care
Tramadol –  moderate to severe  acute intoxication with EtOH/ Fatigue, postural  [1] caution: excessive bronchial secretion, Hx of epilepsy, not for substitute of opioid-dependent
MOR agonist (acute pain) analgesics/ hypnotics/ opioids hypotension  P: manufacturer advise avoid; B: amount too small to be harmful (manufacturer advise avoid)
+ inhibit 5HT &  post-op pain  uncontrolled epilepsy  MR formulations: 12-hourly (Tramulief SR, Zydol SR, Tramquel SR); 24-hourly (Zydol XL)
NA reuptake
Meptazinol –  Moderate and severe  MI Arrythmias,  [2] caution: effect only partially reversed by naloxone; n/v more common on initiation
partial agonist pain (including post-op,  Pheochromocytoma dizziness,  Renal: dose may be reduced in moderate to severe RF
of mu opioid renal colic) drowsiness, dry
receptor mouth, n/v
Non-opioid analgesics/ NSAIDs/ migraine
Non-opioid analgesic: paracetamol, NSAIDs, nefopam (no resp S/E, but sympathomimetics & antimuscarinic effect), ziconotide (intrathecal infusion, only used by hospital specialist as adjunct to opioid analgesic)

,Generic name Indications (other CCI (other CCIs in bold) CSE (other S/E) MOA/POI/ BP/ renal & hepatic impairment (other information in bold)
– drug class indications in bold)
Paracetamol  mild to moderate pain  Dose (oral suspension):  MOA: inhibit PG production and inhibit hypothalamic heat-regulating center to allow peripheral
 pyrexia 120mg/5ml 6-year plus (250mg/5ml) vasodilation
2m-3m 2.5ml BD 6-8 5ml QDS  [3] (1) adult max dose 4g/d (2) lower dose for lower weight patients (adult weight 10-50kg 
3m-6m 2.5ml QDS 8-10 7.5ml QDS dose:15mg/kg q4-6h, max 60mg/kg) (3) caution in alcohol dependence, chronic malnutrition,
6m-24m 5ml QDS 10-12 10 ml QDS dehydration
2-4 7.5ml QDS 12-16 10-15 ml QDS  B/P: OK
4-6 10ml QDS ≥16 10-20ml QDS  Renal: Increase infusion dose interval to q6h when eGFR<30
 Overdose:
1) can cause n/v, encephalopathy, hemorrhage, cerebral oedema, lead to hepatocellular
necrosis, renal tubular necrosis
2) antidote: acetylcysteine (most effective when given within 8hrs of ingestion  given in 3
N-acetylcysteine adverse reactions infusions 150mg/kg over 1 hr, then 50mg/kg over 4 hrs, then 100mg/kg over 16hrs) 
1) Anaphylactoid reactions (common in 1st loading dose): n/v, flushing, skin rash, precursor of GSH (glutathionine) that can protect the liver by increasing the non-toxic ulphur
pruritus (severe: angioedema, bronchospasms, resp distress, hypotension) conjugation
abolish by temporarily suspending the infusion then recommence at the lowest 3) assess serum paracetamol level, AST, ALT, arterial pH, lactate level, U&E, RF
infusion rate (asthmatic patients may have increased risk of anaphylactoid reactions) 4) 2 types of overdose:
2) Coagulation: increase/ decrease prothrombin time A) Acute overdose (>150mg/kg in less than 1 hr)  offer activated charcoal (if overdose
3) Fluid & electrolyte: may cause fluid overload leading to hyponatraemia and seizures; occur in the previous hr); offer acetylcysteine if pt at risk of hepatic impairment if plasma
may also cause hypokalaemia paracetamol concentration is at or above the treatment curve of paracetamol overdose
nomogram (from 4 hrs to 24 hrs after ingestion)
RF of paracetamol toxicity: B) ‘staggered’ overdose (with uncertain time of overdose) – involve ingestion of overdosed
1) Taking P450 inducing drugs e.g. C, P, phenobarbitone paracetamol over 1 hr  offer acetylcysteine (unless patient is asymptomatic + normal
2) Hx of self-harm, frequent use of paracetamol LFT, RF, INR + undetectable paracetamol concentration)
3) Glutathione deficiency – acute/ chronic starvation, malnutrition, CF
Ibuprofen –  Mild to moderate pain  Active/Hx GI bleed/perforation  [4] (1) tablet should not be crushed (2) take with food (3) may cause renal impairment (4) caution for PO use: present/
non-selective (migraine, dental, RA, related to NSAIDs use (CCI if Hx Hx of cardiac failure, oedema, asthma, IBD (may be exacerbated), peripheral arterial disease, IHD, uncontrolled HT
COX-I dysmenorrhea, ≥ 2 distinct episodes)  P: avoid; B: caution (too low to be harmful)
postoperative  NSAIDs HS  Hepatic: avoid in severe (increased risk of GI bleed + fluid retention); Renal: avoid in severe (inc topical form)
analgesia)  Severe HF  Specific caution (topical use): avoid close contact with eyes, broken skin, mucous membrane; avoid excessive

,  Pyrexia exposure under sunlight after application due to photosensitivity; large application quantity may result in systemic effect
 Inflammation  Max dose for adult: 2.4g/d
 Dose (oral suspension):
Ibuprofen oral suspension (100mg/5ml)
3m-6m 2.5ml TDS
6m-12m 2.5ml TDS-QDS
1-3 5ml TDS
4-6 7.5ml TDS
7-12 10ml TDS
>12 10-20ml TDS
 Conception: long term use may reduce fertility (reversed by stopping treatment)
 Overdose: can cause n/v, epigastric pain, tinnitus; antidote: activated charcoal
Aspirin –  Mild to moderate pain  NSAIDs HS causing angioedema, Increased  [2] (1) avoid use in gout (aspirin can compete with uric acid for kidney excretion) (2) take with
non-selective  Pyrexia bronchospasm, rhinitis, uritcaria bleeding time, skin food/ use gastro-resistant formulation too reduce GID;
COX-I &  Immediate (Cross HS with NSAIDs: Difflam, HS, GID  P: avoid analgesic dose in the last few weeks of pregnancy (high dose can cause growth
antiplatelet management & 2nd cocillanna compound, restriction, teratogenic effect & caution in antiplatelet dose during 3rd trimester; B: avoid (Reye’s
prevention of thrombotic mesalazine, salicylic acid, syndrome)
events (MI, stroke) sulphasalazine, thymol gargle  Hepatic: avoid in severe (increased risk of GI bleed); Renal: avoid in severe (increase fluid
 Pre-eclampsia (i.e. HT compound) retention)
and proteinuria in  Previous/ current peptic  Caution: anaemia, asthma, G6PD deficiency, thyrotoxicosis
pregnancy, especially ulceration  Overdose: can cause hyperventilation, tinnitus, deafness, vasodilation, sweating & coma (severe);
at from 20 weeks  Children under 16 (Reye’s antidote: activated charcoal (within 1 hr after ingestion) + replace fluid loss + IV NaHCO3 (after
onwards) syndrome) unless for Kawasaki correction of K+ as hypokalaemia can cause urine alkalinisation) to increase urinary salicylate
disease (widespread secretion (pH 7.5-8.5); haemodialysis in severe case
inflammation in blood vessels)  RF of pre-eclampsia: DM, HT, CKD, having other conditions e.g. lupus, anti-phospholipid
 Haemophilia and other blood syndrome, FH, > 40, BMI≥35, twins, first/ multiple pregnancy, pregnancy interval of more than 10
disorders years
 Indomethacin – licensed for the treatment of patent ductus arteriosus (heart disease) in neonates
Naproxen –  Pain and inflammation Same as ibuprofen Skin HS, fluid  [4] (1) tablet should not be crushed (2) may cause renal impairment (3) associated with the lowest
non-selective  Dysmenorrhea retention, GID thrombotic risk compared to other NSAIDs (4) caution: present/ Hx of cardiac failure/ oedema
COX-I  Acute gout  P: avoid; B: caution (too low to be harmful)
 Hepatic: Avoid in severe (increased risk of GI bleed); Renal: avoid when eGFR<30
 Conception: same as ibuprofen
Sumatriptan  Acute migraine  Previous cerebrovascular disease Drowsiness,  [6] (1) caution in sulphonamide HS, elderly, CVD (2) avoid alcohol (3) tablet should not be
–5HT (1B/1D)  Cluster headache  Peripheral vascular disease dizziness, crushed (4) many DIS (5) take 2nd dose after 2 hrs if 1st dose is partially responded (6) don’t take
agonist  Moderate to severe HT dyspnea, transient 2nd dose if 1st dose is not responding
 Ischemic heart disease increase in BP,  P: avoid; B: withhold breastfeeding 12 hrs after treatment
 >65 (unlicensed) flushing, sudden  Hepatic: reduce dose to 25-50mg (avoid in severe hepatic impairment); Renal: caution
heat sensation at  Classifications of triptan (fast onset): sumatriptan, almotriptan, rizatriptan, zolmitriptan,
any part of the eletriptan; (slow onset): frovatriptan, naratriptan
body  Prevention of migraine: considered when (1) pt suffer ≥ 2 attack a month that produce
disability lasing for 3 days or more (2) increasing frequency of headaches (3) having significant
disability despite suitable treatment (4) cannot take suitable treatment
o Med for migraine prophylaxis (unlicensed use): beta blockers (e.g. propranolol, atenolol,
metoprolol, nadolol, timolol), TCA, topiramate, valproates, gabapentin, pizotifen (histamine and
5HT blocker; can cause weight gain), botulinum toxin A
 Standard treatment of cluster headache: sumatriptan SC (alternative: sumatriptan/ zolmitriptan
nasal spray – both unlicensed); Prophylaxis: verapamil, Li, prednisolone (unlicensed)
Neuropathic pain
Generic name Indications (other CCI (other CCIs in bold) CSE (other S/E) MOA/POI/ BP/ renal & hepatic impairment (other information in bold)
– drug class indications in bold)
Amitriptyline  Depression  Immediate recovery period post MI Arrhythmias,  [1] (1) caution in elderly (more prone to S/E)
– TCA (inhibit  Neuropathic pain  Arrhythmias (heart block) antimuscarinic  P: use if +ve>-ve; B: too small to be harmful
NA and 5HT (unlicensed)  Mania effect sedation,  Hepatic: avoid in severe (increase sedation)
reuptake)  Migraine prophylaxis confusion,  Treatment cessation: should gradually withdraw over 4 weeks (6m for long term treatment);
(unlicensed) mydriasis (dilation withdrawal symptoms occur within 5 days of treatment cessation
of pupils)  Overdose: can cause dry mouth, coma, hypotension (due to alpha blockage), hypothermia,
convulsion, resp failure, tachycardia (due to increase level of NA), QRS prolongation (due to
inhibition of Na+/K+ ATPase pump  slow depolarization and propagation of cardiac action
potential); antidote: activate charcoal (within 1 hr) + IV lorazepam/ diazepam for convulsion

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