Clinical pharmacology connects medical practice and laboratory science by promoting drug safety, maximizing therapeutic effects, and minimizing side effects through rigorous evaluation of evidence and clinical studies. Clinical pharmacologists are trained in medicine and science to analyze various aspects of drug action including therapeutics, toxicology, cardiovascular risks, and drug interactions. Clinical pharmacology applies scientific principles to understand how drugs are administered, distributed, metabolized, and excreted in the body and how they act at molecular, cellular, organ system and whole body levels.

1. Clinical Pharmacology

2. Clinical pharmacology
• Clinical pharmacology connects the gap between
medical practice and laboratory science.
• The main objective is to promote the safety of
prescription, maximise the drug effects and
minimise the side effects.
• It is important that there be association with
pharmacists skilled in areas of drug information,
medication safety and other aspects of pharmacy
practice related to clinical pharmacology.

3. Clinical pharmacology
• Clinical pharmacologists usually have a rigorous
medical and scientific training which enables
them to evaluate evidence and produce new data
through well designed studies
• Their responsibilities to patients include, but are
not limited to, analyzing
– Drug therapeutics, toxicology (including reproductive
toxicology), cardiovascular risks, perioperative drug
management (those used in operations),
psychopharmacology, and Iatrogenic effects (adverse
drug effects)

4. Clinical Pharmacology
• Clinical Pharmacology is the subject of the
application of drugs to the body in the
medicinal sense
• Drugs can function either by action through
receptors, or by altering the functions of the
target cell/tissue

5. Principles
of drugs
action

6. Receptors
• One facet of drug action is receptors
– Agonist: do have a stimulatory effect
• They produce a response
– Antagonist: do not have a stimulatory effect
• They do not produce a response, or have an overall blocking action
for a parallel stimulation
• Types:
– Agonist: have a central pore
– G – Protein: usually linked by secondary messengers to
physiological (cellular) processes
– Nuclear receptors for steroid hormones: in cell nucleus
and regulate protein translation and thus synthesis
– Kinase – linked receptors: usually process intrinsic tyrosine
activity (insulin, cytokines, growth factors)

7. Neurotransmitters
• These are substances released from the end of
nerve axons, at synapses, and bind to receptors.
They activate the receptors, by changing their
configuration, and trigger a response in the post-
synaptic membrane. If it is an agonist, it may
stimulate a muscle contraction or gland
secretion.
• After they have produced their effect, they are
inactivated by:
– Postsynaptic enzymic degradation
– Reabsorption into the pre-synaptic bulb

8. Hormones
• These are chemicals that are released into the bloodstream, then
they act on tissues that have receptors for them (see videos):
– Cells a long way away (steroids)
– Cells locally
– Themselves
• Drug Hormone Actions:
– Inhibiting hormone release:
• Antithyroid drugs
– Increasing hormone release:
• Antidiabetic drugs
– Interact with hormone receptors:
• Activating: steroidal anti-inflammatory drugs (NSAI)
• Blocking: oestrogen antagonists
– Local hormones (released in pathological processes):
• Histamine - antihistamine
• 5-HT, kinins
• Prostaglandins – aspirin (NSAI)

9. Synapse - video

10. Drug-receptor interactions
• A drug that has a stimulatory effect is an agonist
• A drug that blocks this activity, or has an inhibitory effect is
an antagonist (a term used in relation to the agonist)
• Antagonists can bind in two ways:
– Competitive antagonists bind reversibly with receptors; tissue
response can be normalised/increased by increasing the dose of
agonist
– Irreversible antagonists bind irreversibly with receptors; their
effect cannot be reversed by increasing agonist dose
– Others:
– Calcium-channel blockers do not via receptors, but further along to
prevent the action of an agonist
– Chemical antagonists bind to the active drug, inactivating it e.g.
Protamine abolishes effect of heparin
– Physiological antagonists are two agents with opposite effects that
tend to cancel each other out e.g. Prostacyclin and thromboxane- A2
on platelet aggregation

11. Neuromuscular
junction

12. ANS

13. Cholinergic Agonists
Distigmine, Pilocarpine (Pilogel, Side Effects
Salagen), Pyridostigmine • Diaphoresis (sweating)
(Mestinon) • Headache
• Urinary Urgency
Effects
• Nausea
Improves muscular contraction
• Diarrhoea
Uses • Hypotension
• Atonic Bladder and Urinary • Salivation
Retention • Flushing
– Postpartum or postoperative • Abdominal Pain and Cramps
• Muscular Weakness • Bronchial Spasms (panting)
– Myasthenia Gravis • Heart Palpitations or Tachycardia
• Ocular Eye Pressure • Tremors
– Glaucoma Interactions with other conditions
• Asthma, hyperthyroid, hypotension

14. NMJ blockers
• Presynaptic exocytosis (block released of
acetylcholine):
– Botulinum toxin (Botox): blepharospasm,
hemifacial spasm (can produce paralysis for about 12 weeks),
wrinkles
– Baclofen (Lioresal) inhibit calcium influx necessary for exocytosis –
usually only NMJ blockers
– Aminoglycoside antibiotics: inhibit calcium influx necessary for
exocytosis – usually only NMJ blockers
– Dantrolene (Dantrium) -Chronic spasticity

15. Competitive NMJ blockers
• Block nicotinic receptors: used by anaesthetists to relax skeletal
muscle during ECT; usually given IV and don’t pass BBB or placenta.
The drug of choice depends upon the side-effects
– Includes:
• Histamine release
• Vagal blockade
• Ganglion blockade
• Sympathomimetic
• Curare (introd 1942; not longer used)
• Gallamine – doesn’t block ganglia, or releases histamine, but causes tachycardia
• Pancuronium – an aminosteroid and blocks muscarinic receptors, causing
atropine-like tachycardia
• Vecuronium and atracurium – commonly used without CVS effect (only
stable when kept cold at low pH, so in body its breakdown does not depend upon
renal/hepatic function, so good for patients with those problems

16. Depolarising NMJ blocking drugs
• Suxamethonium (Anectine)– depolarises the
post-synaptic membrane; initiates brief
contractions, then the block occurs because:
– Inactivation of the voltage sensitive Na channels
– Transforms activated receptors to a ‘desensitised
state’ and unresponsive to ACh.
• Disadvantages:
– Initial muscle RXN may cause damage - pain
– Damage causes K release
– Repeated doses may cause bradycardia in absence
of atropine

17. Potentiating drugs of NMJ
• Neuromuscular transmission can be increased by
anticholinesterases
• They block the break down of acetylcholine and
thus maintain, or potentiate, the effects of nerve
stimulation
• Effective in conditions like myasthenia gravis; an
autoimmune condition with antibodies
competing for receptors
– Neostigmine
– Pyridostigmine (Mestinon)
• Dosage needs to be accurate; overdose can cause xs Ach and a
depolarising block of the NMJ

18. Acetylcholinesterase Inhibitors
e.g. Donepezil (Aricept), Side Effects
Rivastigmine (Excelon),
Pyridostigmine (Mestinon),
• As Cholinergic Agonists
Neostigmine, Galantamine
Uses Interactions with other
• Cognitive Deficit conditions
– Alzheimers
• Constipation
• Attention Deficit (impaired
memory)
– ADHD
• Muscular weakness
– Myasthenia Gravis

19. ANS

20. ANS

21. ANS

22. Drugs acting at cholinergic synapses
• Muscarinic agonists • Nicotinic agonists (ganglion
stimulants)
– Carbechol
– Nicotine
– Pilocarpine (Salagen)
– Carbechol (weak)
– Bethanechol
– Anticholinesterases (weak)
• Anticholinesterases
– Edrophonium
• Ganglion blockers
– Trimetaphan
– Neostigmine
– Xs nicotine (depolarising block)
– Distigmine
– Pyridostigmine • Muscarinic antagonists
– (organophosphorus – Atropine
compounds) – Hyoscine
– Ipratropium
– Tropicamide
– Benzatropine
– Others

23. Antimuscarinic Agents – muscarinic blockers
Atropine (Atropine), Benzatropine, • Side Effects
Biperiden, Dicycloverine
– Blurred vision
/Dicyclomine (Merbentyl),
Homatropine, Hyoscine (Buscopan), – Confusion
Oxybutynin (Cystrin, Ditropan), – Drowsiness
Orphenadrine (Biorphen, Disipal),
– Dizziness/Vertigo
Procyclidine (Arpicolin, Kemadrin),
Tolterodine (Detrusitol), – Constipation
Trihexyphenidyl, Trospium – Dry Mouth
Others : Ipratropium Bromide (Atrovent, – Palpitations - Tachycardia
Combivent, Respontin), Oxitropium,
Tiotropium (Spiriva), Baclofen
– Restlessness
(Baclospas, Balgifen, Lioresal), – Headache
Carisprodol, Dantrolene, – Urinary Retention
Methocarbamol
Uses
• GI Tract, Bladder spasms – Irritable
Bowel, Abdominal Pain, Incontinence
• Muscle Rigidity and Spasms –
Parkinsons
• Bronchodilators – Asthma

24. Drugs
acting at
cholinergic
synapses

25. Adrenaline Effects Biological advantage Sensation
High heart beat Sends more glucose & oxygen to Thumping heart
the muscles
High respiratory rate Increased oxygenation of the Panting
blood; rapid removal of carbon
dioxide
Arteriole constriction Blood diverted from skin & Person turns pale
digestive system to muscles
Muscle tension Ready for immediate action Tense feeling; Shivering; Erect
body hair
Glycogen is converted to Glucose available for energy
glucose production
Fats are converted to Muscles contraction
fatty acids

28. ANS- Adrenoceptors
• Adrenoceptors: - two main types: α, β
– α: 2 types:
• α1 – vasoconstriction
• α2 –
– inhibition of insulin release in pancreas
– induction of glucagon release from pancreas.
– contraction of sphincters of the gastrointestinal tract
– negative feedback in the neuronal synapses
– platelet aggregation

29. ANS- Adrenoceptors
– β:- 2 types:
– β1 –
• Increase cardiac output
• raising heart rate (positive chronotropic effect)
• increasing impulse conduction
• increasing contraction thus increasing the volume
expelled with each beat (positive inotropic effect;
increased ejection fraction).
• Renin release from juxtaglomerular cells
• Lipolysis in adipose tissue

30. ANS- Adrenoceptors
• β2 -
– Smooth muscle relaxation, e.g. in bronchi
– Lipolysis in adipose tissue
– Anabolism in skeletal muscle
– Relax non-pregnant uterus
– Relaxes detrussor muscle of bladder wall
– Dilate arteries to skeletal muscle
– Glycogenolysis and gluconeogenesis
– Contract sphincters of GI tract
– Thickened secretions from salivary glands
– Inhibit histamine-release from mast cells
– Increase renin secretion from kidney
– Promotes insulin release from pancreatic beta cells

31. Drugs acting on sympathetic system
Sympathomimetics • Adrenergic neurone blockers
• Indirectly acting – Reserpine
– Ephedrine
– Amphetamine – Guanethidine
– Cocaine – Bethanidine
• Directly acting
• Adrenoceptor antagonists
– α- agonists
– α – Blockers
– α1, α2
• Noradrenalin – α1, α2
• Adrenaline • Phenoxybenzamine
– α2 • Phentolamine
• Clonidine (Catapress)
• α-methyl-noradrenalin – α1
– α1 • Prazosin (Hypovase)
• Phenylephrine • Doxazosin (Cardura)
• Metaraminol
• Guanethidine
• Prazosin
• Terazosin
• Tamsulosin (Flomax)

32. Drugs acting on sympathetic system
Sympathomimetics Side Effects
• Indirectly acting • Diaphoresis (sweating)
• Headache
– Ephedrine
• Palpitations
– Amphetamine • Fatigue
– Cocaine, • Angina
– Methamphetamine • Depression
• Hypotension
– Dex(tro)amphetamine
• Hypertension
– Methylphenidate (Ritalin) • Dry Mouth
– Modafinil • Nausea and Vomiting
– Uses • Poor Appetite
– Obesity • Diarrhoea
• Abdominal Cramps
– Somnolence
• Overdose – restless, irritable, insomnia,
– ADHD dizziness, tremors, talkative, fever, anxiety,
– Sleep Apnea panic, confusion, delirium, hallucinations,
– Fatigue aggressiveness, psychosis,
suicidal/homicidal thoughts, convulsions,
– Recreational Drugs coma, cerebral haemorrhage
• These drugs should not be used
concurrently with MAOI’s

33. Adrenergic (alpha) blockers
• Doxazosin (Cardura), Side Effects
Guanethidine, Prazosin, • Postural Hypotension
Terazosin, Tamsulosin
(Flomax), Bethanidine, • Nausea and Vomiting
Phenoxybenzamine, • Nasal Congestion
Phentolamine • Fatigue
• Uses • Headache
– Hypertension • Poor Ejaculation
– Prostatic Hypertrophy • Palpitations - Tachycardia
– Relieves constriction of • Oedema
Bladder and Prostrate
sphincters

34. Adrenergic β agonists
– β- agonists – β- blockers
– β1, β2 – β1, β2
• Adrenaline
• Propranolol (Inderal)
• Isoprenaline
• Timolol (Moducren)
– β2
– β1 (cardioselective)
• Salbutamol
• Terbutaline • Metoprolol (Betaloc,
– β1 Lopressor)
• Noradrenalin • Atenolol (Atecor)
• Dobutamine

35. Adrenergic β agonists
Adrenaline, Isoprenaline, Side effects
Salbutamol, Terbutaline, • Tachycardia
Noradrenalin,
• Arrhythmias
Dobutamine, Xamoterol
Uses • Hypertension
• Congestive Heart failure • Angina
• Bradycardia
• Asthma
• Anaphylaxis

36. Drugs acting
on
sympathetic
system

37. Managing hypertension
• Usually done with a combination of factors;
– Blood pressure reduction
– Diuretics
– Cholesterol
– Anxiety

38. Blood pressure
Drug groups used to control blood pressure:
• β Blockers
• Diuretics
• Calcium channel blockers
• Angiotensin converting enzyme (ACE) inhibitors
• Angiotensin II receptor blockers (ARBS)
There is no reliable/consistent evidence indicating
substantive differences between drugs classes in the
effects on BP, but side effects profiles of each drug
class differ.

39. Beta Blockers
Atenolol (Antipressan, Beta Adalat, Side Effects
Tenormin, Tenoret), Betaxolol, Bisoprolol, • Heart Palpitations – Bradycardia
Celiprolol, Esmolol, Metoprolol (Betaloc, • Hypoglycaemia (reduced glycogenolysis)
Lopresor), Nebivolol (Nebilet), Acebutolol,
Carvedilol, Labetalol, Nadolol, Pindolol, • Bronchoconstriction
Propranolol (Cardinol,Inderal), Sotalol • Insomnia
(BetaCardone,Sotacor), Timolol (Betim, • Nightmares
Prestim, Timoptol) • Depression, Fatigue
Action - Cardiac Selective and Non Cardiac • Cold Extremities
Selective. • Peripheral Vascular Disease
• Beta blockers counteract the action of • Reynaud's Syndrome
noradrenalin, and reduce the force and
speed of the heart beat. Non Cardiac • Decreased Libido and Ejaculation
Selective drugs also prevent dilation of Problems
blood vessels in the head and extremities. Contraindications
Uses • Bradycardia
• Hypertension • Hypotension
• Migraines • Metabolic acidosis
• Hyperthyroidism • Peripheral arterial disease
• Angina • Heart block/failure
• Myocardial Infarction • Phaeochromocytosis
• Bronchial asthma

40. Diuretics
• Aldactide, aldactone, Centyl, Side effects
dyazide, fruside, lasix, moduret, • Headaches
natrilix, napamide, natrilix, • Dizziness
Actions • Fatigue
• Reduce volume in cardiovascular • Urinary tract obstruction
system
• Postural hypotension
Uses
• GIT disorders
• Hypertension
• Electrolyte disturbances
• Polyuria
• Muscle cramps
• Tinnitus

41. Calcium channel blockers
• Nifedipine (adalat), Diltiazem Side effects
(adizem), amlid, amlist, amlode, • Ankle swelling
amlotan, diltam-retard, dilzem,
entrydil, exforge, myostin, nifed, • Headache
nivadil, plendil, rustin, tildiem,
triapin, tritace, verap, verisop, • Flushing
zanidip, • Palpitation
Actions
• Presynaptic neurone blocker • Nausea/dyspepsia
Uses • Abdominal pain
• hypertension
• Dizziness
• Lethargy

42. ACE inhibitors
• Accupro, accuretic, aceomel, Side effects
bitrite, capoten, captor, carace,
• Headache
coversil-arginine, cozaar, enap,
geroten, gopten, innovace, • Dizziness
lisopress, lispril, loavel, odrik, • Rhinitis/cough
pendrex, ramic, ramilo, ramitace, • Upper respiratory tract infection
vascace, zesger, zestan, zestril, • Fatigue
zofenil
• Nausea
Actions
• Dyspepsia
Inhibits conversion of angiotensin I
• Myalgia
to angiotensin II
• Chest/abdominal pain
Uses
• Hypotension
• Hypertension
• Angioedema

43. Angiotensin II blockers
• Aprovel, atacand, • Side effects
benetor, beta-adalat, • Chest/back/abdominal
diovan, isoptin, istin, pain
micardis, omesar, • Arthralgia
teveten,
• Fatigue
Actions
• Dyspepsia
• Causes vasodilatation,
blocks vasopressin • Rhinitis/pharyngitis
release • Dyspnoea
Uses • Upper RTI/viral
• Hypertension • Headache
• Dizziness

44. Antihypertensive
drugs

45. Angina Drugs
• Short acting nitrates
– Glyceryl trinitrate (Glytrin, Nitrolingual)
• Long acting nitrates
– Isosorbide (Elantan, Imdur, Isomel)
• Calcium antagonists
– Nifedipine (Adalat, Nifed)
– Amiodipine (Amid, Amiotan)

46. Cardiac Arrhythmias
• Anti-Arrhythmics Side Effects
Sodium Channel Blockers: Disopyramide, • Potential exacerbation of arrhythmias
Flecainide, Phenytoin (Epanutin), • Flecainide, Propafenone – Dizziness,
Procainamide, Propafenone, blurred vision, headache, nausea,
ventricular tachycardia
Quinidine
• Amiodarone – interstitial pulmonary
Potassium Channel Blockers: fibrosis, tremors, ataxias, dizziness,
• Amiodarone (Cordarone), Sotalol thyroid and liver disease, photosensitivity,
(Beta Cardone, Sotacor) muscle weakness, neuropathy
• (Also Beta Blockers, Calcium Channel • Disopyramide, Quinidine – dry mouth,
Blockers, Inotropic Agents – see urinary retention, blurred vision,
constipation
sections)
• Quinidine – may cause SA or AV node
Uses block, ventricular tachycardia, nausea,
• Arrhythmias e.g. atrial fibrillation or vomiting and diarrhoea, blurred vision,
flutter, ventricular fibrillation, tinnitus, headache, disorientation,
atrioventricular blocks, sinus psychosis
arrhythmias, Palpitations – • Procainimide – erythema, ventricular
Bradycardia, Tachycardia arrhythmias, depression, hallucination,
psychosis
• Impulse tramissions from other than
the sinoatrial node – e.g. potassium
imbalance in other cardiac cells

47. Heart failure
• Inotropic agents • Diuretics
– Digoxin – Bendroflumethiazide
– Dobutamine (Centyl K)
• β- Blockers – Bumetanide (Burinex)
– Carvedilol (Eucardic) – Furosemide (Frumil)
– Bisoprolol (Cardicor) • Aldosterone antagonist
– Metoprolol (Betaloc) – Spironolactone
(Aldactide)
• ACE inhibitors
– Captopril (Capoten)
– Enalapril (Innovace)

48. Cholesterol reducing drugs (Statins)
• Atorvastatin (Lipitor), Fluvastatin, Side Effects
• Muscle Cramps
Lovastatin, Pravastatin (Lipostat),
• Abnormal Liver Function Tests
Rosuvastatin (Crestor), • Steatosis (Fatty Liver)
Simvastatin (Vytorin, Zocor) • Pancreatitis, Hepatitis, Jaundice
Action • NAFLD (Non Alcoholic Fatty Liver Disease)
• NASH (Non Alcoholic Steatotic Hepititis)
• Reduce LDL and VLDL Cholesterol • Cirrhosis
by inhibiting HMG-CoA enzyme • Muscle Wastage – Rhabdomylosis (raised serum
used to produce cholesterol in creatine ->urine)
• Acute Kidney Failure (peripheral oedema,
the Liver, and so reduce release weight gain, poor appetite,
into the Bloodstream. • weakness, nausea)
Uses Precautions
• Not to be used with concurrent Liver Disease or
• Hyperlipidemia (High Cholesterol) the Oral contraceptive. Liver function tests
must be performed before administration and
Also repeated regularly during treatment. Creatine
• Cholesterol absorption inhibition Phosphokinase (CPK) levels should be
performed in anyone with kidney impairment,
– Ezetimibe (Ezetrol)- used in hypothyroid disorder, inherited muscle
combination with statins disorders, previous muscle toxicity in
conjunction with statin use or alchohol abuse

49. Fibrates/Bile Sequestrants/Lipase Inhibitors
• (Questran), Colestipol, Ezetimibe Ezetimibe inhibits cholesterol absorption
(Vytorin, Zetia), Niacin (Advicor, from the gut. Again the Liver
Niacor,Niaspan), Omega 3 Acid responds by increasing LDL uptake
from the blood.
Ethyl Esters (Omacor), Orlistat
(Zenical) Niacin acts on adipose tissue and blocks
formation of fatty acids to circulate in
Bile Acid Sequestrants bind with bile the blood to the Liver for repackaging
acids and salts from the into LDL.
GallBladder in the SI and cause Uses
their excretion. The Liver then • Hyperlipidemia (High Cholesterol)
takes up more LDL from the blood
Side Effects
to compensate for lack of dietary
• BAS – Nausea, Flatulence,
input, and also causes increased
Constipation, interferes with
bile acid production to take more absorption of fat soluble vitamins A D
cholesterol from the gut. E and K
Fibrates cause an increase in • Fibrates – cholelithiasis, muscle
lipoprotein lipase which breaks inflammation and pain and muscular
down VLDL and promotes storage weakness
of fatty acids in adipose and other • Niacin – skin flushing, burning and
tissues. itching, nausea, abdominal pain,
hyperuricemia, and gout

50. Lipid lowering
drugs

51. Blood coagulation – DVT etc
• Anticoagulants: • Anti-platelet:
– Vitamin K antagonist – Aspirin
• Warfarin (Warfant) – Angina, MI
– Heparin – Clopidogrel (Plavix) if
– DVT, CVA, MI aspirin C/I
– Bemiparin (Zibor) – Tirofiban (Agrastat)
– Enoxaparin (Clexane) – Eptifibatide (Integrillin)
• Fibrinolytics: – Abciximab (Reopro)
• Myocardial infarction – Dipyramidole (Persantin)
– Prosthetic heart valves
– Streptokinase
– Alteplase (Actilyse)
– Reteplase (Rapilysin)

52. Anticoagulants
• Abciximab, Aspirin (Caprin, Disprin, Side Effects
Nuseal, Anadin), Clopidogrel (Plavix),
Dipyridamole (Persantin, Asasantin), • Prolong bleeding times:
Eptifibatide, Ticlopidine, Tirofiban Haemorrhage, GI Bleeding,
• Other : Warfarin (Marevan, Thrombocytopenic Purpura
Coumadin)
Actions • Warfarin – pain and
• Prevent platelet aggregation and swelling, headaches,
coagulation reactions - venous dizziness, weakness,
thrombosis, pulmonary embolism
and thrombo embolisms.
unusual bruising, nose
Uses bleeds, bleeding gums,
• Angina heavy menstrual bleeding,
• Myocardial Infarction brown or pink urine, red or
• Prevention of cardiovascular black stools, coughing or
occlusion – DVT/embolism vomiting blood
• Transient Ischemic Attacks (TIA’s)

53. Drugs affecting blood
coagulation

54. Agents used in anaemia
• Fe preparation (increases Fe available)
– Oral:
• Ferrous sulphate
• Ferrous gluconate
• Ferrous fumarate
– Parenteral
• Iron dextran (ferric hydroxide)
• Iron sucrose (ferric hydroxide)
• Vitamins (important for normal blood production)
– B12, B9 (folate)
• Erythropoietin (produced by the peritubular capillary
endothelial cells in the kidney; stimulates
erythropoiesis in bone marrow - If renal failure)

55. Agents used in anaemia

56. Ocular pharmacology
• Glaucoma
β – Blockers (reduce aqueous humour production)
• Betaxolol (Betoptic)
• Cartelol (Teoptic)
• Timolol (Nyogel)
Prostaglandin analogues (increase uveoscleral outflow)
• Latanoprost (Xalatan)
• Bimatoprost (Ganfort)
Carbonic anhydrase inhibitors (reduce aqueous humour production)
• Acetazolomide
• Dorzolamide
• Brinzolamide
Sympathomimetic (reduces production aqueous humour and outflow)
• Adrenaline, guanethidine (Ganda)
• Brimonidine (Alphagan)
• Age related macular degeneration
– Verteporfin (Visudyne)

57. Ocular
pharmacology

58. COPD (asthma/bronchitis/emphysema/cystic fibrosis etc)
• Bronchodilators – Side effects (brochodilators)
• Tremor
(COPD) (Relievers)
• Tachycardia
– β2 agonists • Headache
• Salbutamol (Ventolin) • Hypokalaemia
• Terbutaline (Bricanyl) • Steroids (Preventers)
– Muscarinic blockers – Beclomethasone (Becotide)
• Ipratropium (Atrovent) – Serotide (salmetrol and
– Combinations fluticasone)
• Salbutamol, Ipratropium Side effects
(Combivent) • Hoarseness
– Xanthines • Candidiasis of mouth
• Aminophylline
(Phyllocontin)

59. Hay fever (rhinitis) and Anaphylaxis
Antihistamines: Side Effects
Non-sedating - Acrivastine, Cetirizine • Fatigue
(Benadryl, Piriteze), (Des)Loratidine • Drowsiness
(Clarityn), Fexofenadine, Levocetirizine, • Sedation
Mizolastine
• Hypotension
Sedating – Alimemazine, Azatadine,
Brompheniramine, Chlorphenamine • Dry mouth and eyes
(Piriton, Contac 400, Tixylix), Cinnarizine • Palpitations – Tachycardia
(Cinaziere, Stugeron), Clemastine, • Vertigo
Cyclizine, Diphenhydromine, • Hunger
Diphenylpyraline, Hydroxyzine, Meclozine, • Urinary Retention
Promethazine (Phenergan, Sominex, Night
Nurse, Pamergan, Tixylix Night Time),
Triprolidine Overdose
• Sodium Chromoglycate (Intal) • Hallucinations
– Mast cell stabiliser; reduces • Convulsions
histamine release in allergic asthma • Ataxia
Uses • Coma
• Allergic Rhinitis • respiratory and cardiac collapse
• Dry out mucous membranes
• Motion Sickness
• Insomnia

60. Asthma hay fever and
Anaphylaxis

61. Drugs on GIT 1
Antacids • Helicobacter pylori eradication
– NaHCO3
– CaCO3
– Triple therapy
– Mg(OH)2 • Omeprazole (Losec)
– Al(OH)3 • Clarythromycin (Klacid)
Acid secretion reducers • Amoxicillin (Amoxil)
– Proton pump inhibitors • Omeprazole (Losec)
– Lanzoprazole (Zoton) • Amoxicillin (Amoxil)
– Omeprazole (Losec)
• Metronidazole (Flagyl)
– H2 anatogonists
– Cimetidine (Cedine) Side effects
– Rantidine (Zantac)
– Famotidine • Nausea
– Nizatidine • Diarrhoea
– Esomaprazole
Mucosal strenghteners • Headache
• Sucralfate (Antepsin) • Dizziness
• Bismuth chelate • Muscle Pain
• Misoprostal (Cytotec) • Uterine Contractions
Uses
• Reduces secretion of Gastric Acid
• Peptic Ulcers
• Duodenal Ulcers
• Gastro-oesophogeal Reflux

62. Drugs on GIT 1 –
peptic ulcer

63. Drugs on GIT 2 – motility and secretions
• Crohn's disease, ulcerative colitis • Gallstone dissolvers
• Anti-inflammatory – Bile acids
– Corticosteroids • Ursodeoxycholic acid
• Hydrocortisone • Antispasmodics (smooth M relaxants)
• Prednisolone (Predenama) – Muscarinic agonists
– Aminosalicylates • Alverine (Spasmonal)
• Sulphasalazine
• Mebeverine (Colofac)
• Mesalazine (Asacolon, Mezavant)
• Peppermint oil (Colpermin)
• Laxatives
– Bulk
• Antimotility drugs (Poss with rehydration)
• Bran – Morphine-like agents
• Ispaghula (Fibrogel) • Morphine
– Osmotic • Codeine
• MgSO4 • Diphenoxylate, Atropine
• Lactulose (Lomotil)
– Stimulant • Loperaminde (Imodium)
• Senna • Motility stimulants (DA agonists)
• Bisacodyl (Dulcolax) – Metoclopramide
• Co-Danthromer (Codalax)
– Domperidone
• Glycerol (suppositories)
• Pancreatic supplements
– Faecal softeners
• Docusate
– Pancreatin (Nutrizyme)
• Arachis oil (enema)

64. Diarrhoea
• Diphenoxylate (Lomotil), Kaolin, Side Effects
Loperamide (Diocalm, Imodium, • Abdominal Distension and
Diareze, Arret), Methylcellulose Cramps
(Celevac) • Flatulence
Actions • Bloating
• Opioid drugs to decrease muscle • Constipation
propulsion in the bowel by
working on local opioid receptors • Fatigue
in the bowel and slow the • Drowsiness
intestines. Bulk forming agents • Dizziness
absorb water and irritants in the • Itching
bowel and produce larger and • Rashes
firmer stools.
• Dry Mouth
Uses
Precautions
• Diarrhoea
• Not to used in cases of colitis
• Can affect absorption of other
drugs

65. Constipation
Also
• Bisacodyl, Glycerol, Senna, Sodium • Bulk
Picosulfate, Lactulose (Duphalac, – Bran
Regulose), Magnesium Citrate, – Ispaghula (Fibrogel)
• Osmotic
Magnesium Hydroxide (Milk of
– MgSO4
Magnesia, Maalox, Mucogel), – Lactulose
Magnesium Sulphate, Polyethylene • Stimulant
Glycol (Liquid Paraffin) (Glycolax) – Senna
– Bisacodyl (Dulcolax)
Actions – Co-Danthromer (Codalax)
• Stimulants irritate the GI tract and – Glycerol (suppositories)
• Faecal softeners
increase peristalsis for directly
– Docusate
stimulate colon activity. Softening – Arachis oil (enema)
agents emulsify the stool. Osmotic Side Effects
laxatives cause water to stay in the • Flatulence
• Belching
intestines
• Stomach and Abdominal Cramps
Uses • Diarrhoea
• Nausea
• Constipation
• Abdominal Distension
• Osmotic laxatives can cause electrolyte imbalances

66. Irritable bowel disease/syndrome
• Aminosalicylates : Balsalazide, Side Effects
• Nausea and Vomiting
Mesalazine (Asacol, Pentasa,
• Malaise
Salofalk), Olsalazine (Dipentum), • Poor Appetite
Sulfasalazine (Salazopyrin, • Diarrhoea
Sulazine, Ucine) • Headaches
• Abdominal Pain
Actions
• Joint Pain
• These drugs block production of • Tinnitis
prostaglandins and other • Insomnia
chemicals that promote • Fatigue
• Fever
inflammation in the bowel
• Rash
Uses • Sore Throat
• Ulcerative Colitis • Haemmorhage
• Erythema Nodosum
• Crohn’s disease • Hypertension
• Palpitations
• Pancreatitis
• Liver problems

67. Drugs on
GIT 2 –
motility and
secretions

68. Drugs acting on kidney - Diuretics
• Thiazides (distal tubule, inhibits • Carbonic anhydrase
Na reabsorption)
inhibitors (weak – rarely used)
– Bendroflumethiazide
– Acetazolamide
(Centyl)
– Indapamide (Natrillix) • Aldosterone
• Loop agents (inhibit Na/K/Cl • Potassium sparing
reabsorption in ascending loop of Henle, diuretics (act on distal nephron;
so no water) reduces Na reabsorption, so spares K)
– Furosemide (Lasix) – Spironolactone
– Butemamide (Burinex) (Aldactone)
– Amiloride
– Triametarene

69. Drugs acting on kidney - Diuretics
• Thiazides Side Effects
– Bendoflumethiazide (Inderex, Inderetic, Prestim),
Chlorthalidone, Cyclopenthiazide, • Thiazides/Loop Diuretics
Hydrochlorothiazide (Acezide, Capozide, Co-
Betaloc, Dyazide, Moduretic), Indapamide
• Hyponatremia – lethargy, muscle
(Natrilix, Coversyl Plus), Metolazone, Xipamide cramps, dizziness, hypotension,
Action confusion, palpitations, fainting
• Inhibit the Na+ transporters in the • Hypokalemia – diet (bananas, citrus
proximal and distal tubules, which allows fruits, prunes) - Muscle weakness,
more water to stay in the tubules. These fatigue, dizziness, confusion, cardiac
diuretics loose efficiency with decreased
arrhythmias, constipation
kidney function. They cause loss of
potassium and magnesium, and cause • Hyperuricemia – gout
increased calcium reabsorption. • Hyperlipidemia – high cholesterol
Uses - broad • Hyperglycemia – increased blood
• Premenstrual Oedema (severe) sugar (danger for diabetics)
• Oedema Precautions
• Ascites
• Can decrease effectiveness of
• Congestive Heart Failure
anticoagulants
• Nephrotic Syndrome
• Can’t be used with low potassium,
cirrhosis, Addison’s or with Lithium

70. Drugs acting on kidney - Diuretics
• Loop Diuretics Side effects
– Bumetanide (Burinex), Furosemide/Frusemide
(Co-Amilofruse, Lasix, Frusol, Frumil, Lasikal), • Hyponatremia – lethargy, muscle
Torasemide cramps, dizziness, hypotension,
Actions confusion, palpitations, fainting
• Loop diuretics work in the Loop of Henle
(which accounts for 25-30% of all NaCL • Hypokalemia – diet (bananas,
reabsorption) again inhbiting the Na+ citrus fruits, prunes) - Muscle
transporters. They cause loss of weakness, fatigue, dizziness,
potassium and magnesium but leave confusion, cardiac arrhythmias,
calcium levels unchanged.
constipation
Uses
• Pulmonary Oedema • Hyperuricemia – gout
• Hyperkalemia • Hyperlipidemia – high cholesterol
• Hypercalcemia • Hyperglycemia – increased blood
Broad uses sugar (danger for diabetics)
• Premenstrual Oedema (severe)
• Oedema
• Ascites
• Congestive Heart Failure
• Nephrotic Syndrome

71. Drugs acting on kidney - Diuretics
• Potassium Sparing Side effects
– Amiloride (Amilamont, Amilospare,
Burinex, Co-Amilofruse, Moduretic),
• Peptic ulcers
Spironolactone, Triamterene (Dytac, • Infertility – sperm and egg
Dyazide, Frusene, Triamax, Kalspare) abnormalities
Actions • Nausea
• Potassium sparing diuretics work in the • Lethargy
collecting tubule and inhibit Na+
reabsorption there as with other diuretics • Confusion
but also prevent potassium excretion. • Leg Cramps
They are not strong diuretics but are often • Increased Blood Urea Nitrogen
used alongside others to prevent
potassium loss. • Increased Uric Acid
Uses • Hyperlipidemia
• Premenstrual Oedema (severe) • Hyperkalemia – tiredness, confusion,
• Oedema muscle weakness, irregular pulse,
• Ascites muscular paralysis, cardiac
• Congestive Heart Failure arrhythmias, cardiac arrest.
• Nephrotic Syndrome

72. Drugs
acting on
kidney -
Diuretics

73. Central transmitter substances
Fast point to point signalling Slow, regulatory, signals
• Acetylcholine (nicotinic effects) • Neuropeptides (over 40 of these)
– Substance P
• Amino acids
– Met-enkephalin
– Glutamate (excitatory)
– Leu-enkephalin
– Aspartate
– Angiotensin
– GABA (inhibitory)
– Somatostatin
– Glycine
– LH releasing H
– Calcitonin gene-related peptide (CGRP)
– Others
• Monoamines
– Dopamine
– Nor-adrenalin
– Adrenalin
– Serotonin (5HT)
– Acetylcholine (ACh)
excitatory/muscarinic. Loss of cholinergic
pathways important in Alzheimer's
• Donezepil
• Rivastigmine
• Nitric oxide

74. Central transmitter
substances

75. Antiepileptic drugs

76. Antiepileptic drugs
• Generalised (tonic-clonic) • Status epilepticus iv
and partial seizures – Lorazepam (Ativan)
– Carbamazepine (Tegretol) – Diazepam (Valium, Anxicalm)
– Valproate (Epilim) – Phenytoin (Epanutin)
– Phenytoin (Epanutin) • General anaesthetics
– Lamotrigine (Lamictal, – Propofol (Diprivan)
Lamoro) – Thiopental
– Topiramate (Topamax) • Absences
– Phenobarbital (also sedative) – Ethosuximide
– ‘Add ons’ if epilepsy not controlled:
– Valproate (Epilim)
– Vigabatrin (Sabril)
– Gabapentin (Neurontin,
• Grand mal and absences
Gabin) – Valproate (Epilim)
– Tiagabine (Gabitril) – BDZ: Clonazepam (Rovotril)

77. Drugs for Parkinson’s Disease
• Aetiology • COMT inhibitor
– Mostly unknown – Entacapone (Comptess)
– Toxin induced (via MPTP, Carbon
monoxide, Manganese) • Dopaminergic drugs:
– Drug induced – DA precursor
• Neuroleptics • Levidopa (Madopar)
• Dopamine antagonists
• (+Carbidopa (Sinemet) or
• Antimuscarinic drugs Benserazide)
– Muscarinic antagonists – Releases DA
• Benzatropine • Amantadine (Symmatrel)
• Procyclidine (Kemadrin) – DA agonists/ergot derivatives
• Orphenadrine • Bromocriptine (Parlodel)
• MAO inhibitors • Carbergoline (Carbaser,
– Selegiline (Eldepryl) Dostinex)
• Pergolide (Celance)
– Non-ergot derivatives
• Ropinirole (Adartrel, Requip)
• Pramipexole (Mirapexin)

78. Parkinson’s Drugs
• Entacapone (COMT), Amantadine Side Effects
(Symmetrel), Bromocriptine • Hallucinations (Visual, Auditory)
(Parlodel), Cabergoline, Lisuride, • Dyskinesias (too much activation
Pergolide, Pramipexole (Mirapex), of CNS)
Ropinirole (Requip),
Levodopa/Carbidopa (Sinemet) Also:
COMT (catechol-O-methyl • Levodopa/COMT - Tachycardia,
transferase) Inhibitor – inhibits hypotension, brown urine,
enzyme that breaks down anxiety, depression, poor
Dopamine and Levodopa appetite, nausea, vomiting
Dopamine Receptor Agonists – • Dopamine Agonists – nausea,
activate Dopamine receptors fatigue, sleepiness
artificially instead of Dopamine. • Amantidine – restlessness,
The mechanism of action of dizziness, agitation, confusion,
Amantadine (an antiviral agent postural hypotension, urinary
against Influenza A) is unknown. retention, peripheral oedema,
Levodopa/Carbidopa - precursor of toxic psychosis (mania)
Dopamine and Carbidopa is a
drug that helps it to be absorbed.

79. Drugs for Parkinson’s
Disease

80. Antipsychotic drugs (neuroleptics)
Phenothiazines; with side chain: Others:
• Propylamine • Butyrophenones
– Chlorpromazine (Clonactil) – Haloperidol (Haldol, Serenace)
• Very sedative • Atypical drugs
• Moderate anticholinergic and
extrapyramidal effects – Clozapine (Clozaril)
• Piperidine – Risperidone (Risperdal,
perdamel)
– Thioridazine
– Sulpiride (Dolmatil)
• Moderately sedative
• Very anticholinergic and fewer
extrapyramidal effects
• Piperazine
– Fluphenazine (Modicate)
– Trifluoperazine (Stelazine)
• Less sedative
• Less anticholinergic and more
pronounced extrapyramidal
effects

81. Neuroleptics (antipsychotics)
Typical Neuroleptics – Side Effects
• Phenothiazines – Chlorpromazine (Chloractil, Largactil),
Flupentixol (Fluanxol), Fluphenazine, • Parkinsonian Effects – loss of balance,
Methotrimeprazine, Pericyazine, Perphenazine,
Pipotiazine, Prochlorperazine (Buccastem, Proziere,
tremors, tardive dyskinesias
Stemetil), Thioridazine, Trifluoperazine; Benperidol, • Blurred Vision
Haloperidol (Haldol, Serenace), Pimozide, (Ami)Sulpride
(Dolmatil, Sulptil), Zuclopenthixol • Dry Mouth
Atypical Neuroleptics -
• Aripipazole (Abilify), Carbamazepine (Tegretol, Teril,
• Sedation
Timonil), Clozapine (Clozaril), Olanzapine (Zyprexa), • Confusion, Constipation
Quetiapine (Seroquel), Risperidone (Risperdal), Zotepine
(Zoleptil) • Urinary Retention
Actions
• All these drugs block DA receptors (opposite of
• Drowsiness
antiparkinsonian drugs). Atypical neuroleptics also block • Postural Hypotension
5HT receptors
Uses • Dizziness, Fainting
• Delusions, hallucinations, disorganised or catatonic
speech or behaviour :
• Amenorrhea
– Schizophrenia, Schizophreniform Disorder, • Infertility, Impotence
Schizoaffective Disorder, Delusional Disorders,
Psychotic Disorders e.g. Personality Disorders, • Significant Weight Gain
Mania
– Aggressive behaviours of Autism
• Neuroleptic syndrome – muscle
– Tourette’s syndrome (Pimozide) rigidity, fever, stupor, unstable blood
– Anti-emetics pressure
• Seizures

82. Antipsychotic drugs
(neuroleptics)

83. Anxiolytics and hypnotics
• Anxiolytics • Hypnotics
– Benzodiazepines BDZ – BDZ (central depressants)
(central depressants)
• Temazepam (Tenox)
• Diazepam (Valium) (seizures)
• Lormetazepam
• Lorazepam (Ativan)(seizures)
(Noctamid)
• Alprazolam (Xanax)
• Nitrazepam (Mogadon)
– Antidepressants
• Amitriptyline
– Others
(depression/anxiety) • Zopiclone (Zimovane)
• Buspirone (anxiolytic) • Chloral hydrate
• Citalopram (Cipramil)(panic • Clomethiazole
disorders) (Heminevrin)
– β – Blockers • (Barbiturates) not used
much because of dependence
• Propranolol

84. Anxiolytics
Side effects
Benzodiazepines (BDZ)
• Amnesia (anterograde and retrograde)
• Alprazolam (Xanax)
• Drowsiness
• Chlordiazepoxide (Librium) • Lack of coordination
• Clonazepam (Klonopin) • Libido/erection problems
• Diazepam (Valium) • Disinhibition/euphoria
• Lorazepam (Ativan) • Confusion
Action • Blurred vision
Herbal treatments
• Acts on GABA : BDZ receptor Cl- channel
complex; this increases the duration of • Certain herbs are reputed to have anxiolytic
properties, including the following:
chloride ion channel opening at the
• Rhodiola rosea (Arctic Weed/Golden Root)
GABAA receptor, thus increases the
• Bacopa monnieri (Brahmi)
efficacy of GABA . By increasing the
available amount of GABA typically have • Hypericum perforatum (St. John's Wort)
relaxing, anti-anxiety and anti-convulsive • Matricaria recutita (German Chamomile)
effects • Mitragyna speciosa (Kratom)
• Piper methysticum (Kava)
Uses
• Sceletium tortuosum (Kanna)
• Panic/anxiety disorders
• Scutellaria spp. (Skullcap)
• Insomnia • Valeriana officinalis (Valerian)
• Seizures • Cannabis sativa (Marijuana)
• ‘muscle relaxant’

85. Anxiolytics and
hypnotics

86. Antidepressants
• Tricyclics
– Amitriptyline(Elavil, Tryptizol, Laroxyl)
Side effects
– Clomipramine (Anafranil) • dry mouth
– Dosulepin (Prothiaden, Dolthep) • dry nose
– Lofepramine (Gamanil)
• blurry vision
• SSRI
– Citalopram (Cipramil)
• lowered gastrointestinal motility
– Fluoxetine (Prozac) or constipation
– Paroxetine (Seroxat) • urinary retention
Actions • cognitive and/or memory
• Block reuptake of Noradrenalin abd impairment
serotonin (5HT) and antagonise many
other receptors (causing side effects) • Increased body temperature
Uses • Drowsiness
• Depression • anxiety
• Bipolar disorders
• Anxiety
• emotional blunting
• Social phobia • Confusion

87. Antidepressants
MAOI’s (monoamine oxidase Side effects
inhibitors)
• Sleep disturbances
• Isocarboxazid (Marplan)
• Moclobemide (Aurorix, Manerix) • Nausea
• Phenelzine (Nardil) • Dizziness
• Selegiline (Eldepryl, Emsam) • Sometimes headaches
• Tranylcypromine (Parnate) • Rarely confusion
Action
• Blocks monoamine oxidase,
which breaks down
neurotransmitters (nor-
adrenaline, dopamine, serotonin)
after presynaptic uptake),
thereby potentiating their effects
Uses
• Depression

88. Antidepressants

89. Lithium
• Camcolit, Priadel Side Effects
Actions • Nausea, Diarrhoea, Drowsiness,
Frequent Urination (polyuria),
• Largely unknown. Thought Frequent Thirst (polydypsia),
to work by decreasing Weight Gain, Hand Tremors, Acne
release of NE and DA while Toxic effects
stabilising or even • Should have regular checks of
increasing release of 5HT (in kidney function, urine analysis,
serum urea and creatinine,
animal studies).
thyroid and heart function
Uses • Vomiting, Diarrhoea, Ataxia,
• Mania in bipolar disorders Tremors, Convulsions, Coma,
Confusion, Hyper reflexes,
• Prophylaxis of depression Seizures, Nerve Damage,
• Cluster headaches Hypotension, Albuminuria,
Cardiac Arrhythmias

90. Epileptics/anticonvulsants
• Acetazolamide, Carbamazepine (Tegretol, Teril, Side Effects
Timonil), Clonazepam (Rivotril), Clobazam,
Diazepam (Rimapam, Tensium, Valclair, Valium), • Common are : Nausea and Vomiting,
Gabapentin (Neurontin), Levetiracetam, Headache, Confusion, Hallucinations,
Lamotrignine (Lamictal), Lorazepam (Ativan),
Phenobarbital (Gardenal), Phenytoin (Epanutin), • Also
Piracetam, Primidone (Mysoline), (Sodium) • Sedation, Ataxia
Valproate (Convulex – valproic acid, Epilim, • Penytoin – megaloblastic anemia,
Orlept), Tiagabine, Topiramate, Vigabatrin
hyperglycemia
Actions
• Carbamazapine – stupor, comia,
• Anticonvulsants – bind with sodium or chlorine
channels to slow action potentials. respiratory depression, blurred vision,
• Some antipsychotics also bind with sodium
rashes, liver toxicity, hyponatremia –
channels (Carbamazepine, Lamotrignine) needs frequent blood and liver function
• Some anxiolytics (benzodiazepines – tests when on drug
clonazepam, clorazepate, diazepam, lorazepam) • Phenobartital, Primidone – vertigo,
and barbiturates (Phenobarbital) bind with psychosis, rashes, agitation, confusion
chorine channels
• Valproate – tremors, rashes, alopecia,
• Some drugs increase GABA release – which then
thrombocytopenia, inhibition of platelets,
binds with chlorine channels (Gabapentin) or
interfere with its breakdown (valproate) liver failure
Uses • Lamotrignine – rashes, internal bleeding
• Sedative, anticonvulsant and muscle relaxant • Levetiracetam – insomnia
• Topiramate – somnolence, anxiety, weight
loss

91. Epileptics

92. Opioid analgesics - narcotics
Opioid analgesics Side effects
– Strong
• Morphine • Respiratory Depression – main
• Diamorphine (Heroin)
• Dihydrocodeine (DF118) cause of death in opioid overdose
• Oxycodone (Oxycontin/OxyNorm)
• Tramadol (Zydol)
• Constipation
– Moderate • Sedation
• Codeine
– Endogenous peptides • Menstrual Changes
• Endorphins
• Enkephalins • Nausea and Vomiting
• Actions
• Addiction -
• Acts on morphine receptors (μЌδσ)
• Uses – pain: • Withdrawal symptoms – tearing,
– myocardial infarction runny nose, sweating, yawning,
– sickle cell crisis flushing, palpitations, spasms and
– pre- and postoperatively twitches, shaking fever,
– trauma restlessness, irritability, insomnia
– severe chronic pain, e.g., cancer
– pain from kidney stones
– severe back pain

93. Opioid analgesics

94. Drugs used in nausea and vertigo (antiemetics)
• Dopamine antagonists Side effects
– Prochlorperazine (Stemetil)
• Nausea
– Metoclopramide (Maloxon,
Primperan, Migramax, Paramax) • Indigestion
– Betahistine (Serc), Domperidone • Drowsiness
(Motilium),
• Sedation
• 5HT3 (serotonin) antagonists
– Ondansetron (Zofran, Emital) • Diarrhoea
– Granisetron (Kytril) • Headaches
• Antimuscarinic drugs • Breast Distension
– Hyoscine (Kwells)
• Muscle Spasms/Tremors
• Antihistamines
– Cinnarizine (Stugeron) • Restlessness
– Promethazine (Phenergan) • Reduced Libido
– Cyclizine (Valoid) • Constipation
Uses
• Nausea and Vomiting from:
• Vertigo/Dizziness (Betahistine)
• Gastroentiritis (Domperidone)
• Chemotherapy

95. Drugs used in nausea and vertigo (antiemetics)

96. Non-steroidal anti-inflammatory drugs (NSAI’s)
• Salicylic acid derivatives
– Aspirin Side effects
• Propionic acid derivatives • All NSAIDs (except for Aspirin)
– Ibuprofen (Brufen, Ibugel)
– Fenbufen (Lederfen)
increase likelihood of cardiovascular
– Naproxen (Naprosyn) events, including myocardial
• Others infarctions, CVA’s and worsening of
– Diclofenac (Cataflam, Voltarol)
hypertension.
– Indomethacin (Indocid)
– Nambumatone (Relifex) • All increase GI irritation, ulceration,
– Phenylbutazone haemorrhage, and perforation; can
• Selective COX2 inhibitors
– Etoricoxib (Arcoxia)
also cause Kidney toxicity
– Celecoxib (Celebrex) • Aspirin (high/toxic doses) -
• Analgesic only respiratory paralysis, coma, oedema,
– Paracetamol
Action
hyperkalaemia, anaphylactic shock in
• Block prostaglandin synthesis, thus 15% of patients
reducing inflammation • Mefenamic Acid and Meclofenamate
Uses – severe diarrhoea, bowel
• Inflammation inflammation, haemolytic anaemia
• Fever
• Acetaminophen – skin rash, allergic
• pain
reactions, long term - renal tubular
necrosis, hypoglycaemia, hepatic
necrosis

97. Non-steroidal anti-inflammatory (NSAI’s)

98. Corticosteroids
• Hormones Side effects
– Hydrocortisone [Cortisol, • Stomach upset
Cortisone] (Hydrocortone) • Increased appetite
• Synthetic • Diabetes mellitus
– Prednisolone/prednisone • Immunosuppression
• Osteoporosis
– Methylprednisone (Depo –
• Elevated liver enzymes
mendrone)
• Cushing’s disease
– Betamethasone (Betnesol,
Long term effects
Betnelan)
• hyperglycaemia, insulin resistance,
– Dexamethasone diabetes mellitus, osteoporosis,
– Triamcinolone (Adcortil) anxiety, depression, gastritis, colitis,
Action hypertension, erectile dysfunction,
• Prevents phospholipid release, hypogonadism, hypothyroidism,
reducing prostaglandin synthesis amenorrhoea, retinopathy.
Uses
• Inflammation
• Immunosuppressant

99. Corticosteroids

100. Hyperthyroidism/Thyrotoxicosis
• Methimazole, Carbimazole Side effects
(Neo Mercazole),
• Headache, dizziness,
Propylthiouracil
nausea, rashes, itching,
Actions hair loss, mouth ulcers
• Inhibit formation of T3 • Reduced Immunity
and T4
• Fever
Uses
• Lymphadenopathy
• Hyperthyroid conditions:
(swollen lymph nodes)
• Palpitations,
hypertension, insomnia,
headaches, aversion to
heat

101. Hypothyroidism
• Levothyroxine (Eltroxin), Side effects
• Anxiety
Liothyronine
• Agitation
Actions • Diarrhoea
• Is a synthetic form of T4 • Weight Loss
• Sweating
Uses • Flushing
• Underactive thyroid, • Muscle cramps
manifesting as: weight • Angina
• Palpitations
gain, fatigue, aversion
• Overdose – hyperthyroid! -> in
to cold, cold addition, insomnia, headaches,
extremities, low irritability, aversion to heat,
hypertension
metabolism

102. Thyroid and Anti-thyroid drugs

103. Posterior pituitary drugs
• Desmopressin (Desmotabs, Side effects
Nocutil), Vasopressin (ADH),
Bromocriptine (Parlodel) • Desmopressin – headache,
Actions nausea, vomiting,
• Desmopressin metabolities nosebleeds, stomach pain,
replace Vasopressin and convulsions, thrombosis,
encourage water conservation myocardial infarction
and release of blood coagulation
• Bromocriptine – confusion,
factors. Bromocriptine inhibits
secretion of prolactin from the dizziness, nausea, vomiting,
pituitary gland. headache, constipation,
Uses dyskinesias
• Diabetes Insipidus (Type 1) –
polyuria, and nocturnal enuresis
• High Prolactin levels – infertility
and impotence

104. Sex hormones and drugs
Infertility • Side effects
• Anti-oestrogen
• Headache
– Clomifene (Clomid)
Action • Oedema
• Selective Estrogen Receptor Modulator • Hypertension
(SERM), increasing production of • Nausea and Vomiting
gonadotropins by inhibiting negative
feedback on the hypothalamus • Post menopausal Uterine
• Gonadotrophins Bleeding
– Choriogonadotropin alfa (Ovitrelle) Long term use
– Follitropin alfa, Lutotropin Alfa
(Pergoveris)
• Thromboembolisms
Actions • Myocardial infarction,
• Causes ovulation • Breast/Uterine Cancer
• Androgens
• Raloxifene – hot flushes, leg
– Testosterone (Andropatch) cramps, swollen ankles, leg pain
• Actions swelling and ulcers
• Stimulates leydig cells to synthesize
testosterone
Uses
• Infertility in men

105. Sex hormones and drugs
• Female sex hormones (HRT) Side effects
– Oestradiol (Climera, Evorel) • Headache
– Estradiol, Medroxyprogesterone • Upset stomach, stomach cramps or
(Indivina) bloating
– Medroxyprogesterone (for • Diarrhoea
endometriosis) (Provera) • Appetite and weight changes
– Levonogestrel (emergency • Changes in sex drive or performance
contraception) (Levonelle) • Nervousness
Actions • Brown or black patches on the skin
• Replaces hormones • Acne
Uses • Swelling of hands, feet, or lower legs
• Osteoporosis due to fluid retention
• Menopause symptoms • Changes in menstrual flow
– hot flashes, vaginal dryness, • Breast tenderness, enlargement, or
urinary stress incontinence, chilly discharge
sensations, dizziness, fatigue, • Sudden difficulty wearing contact
irritability, and sweating lenses

106. Sex hormones and drugs

107. Antidiabetic drugs
• Insulin preparations(Type 1 im) • Type 2
• Short acting • Sulphonylureas
– Insulin, rDNA – Glibenclamide (Daonil)
Saccharomyces cerevisiae – Glicazide (Daimicron)
(Actrapid)
– Glimepiride (Amaryl)
– Insulin aspart (Novomix)
– Glipizide (Glibenese)
• Intermediate acting • Glucosidase inhibitors
– Huminil 1
– Acarbose (Glucobay)
– Insuman basal
• Biguanides
• Long acting
– Metformin (Glucophage)
– Insulatard
– Levimir • PPAR gamma antagonists
– Lantus – Pioglitazone (Actos)
– Rosiglitazone (Avandia)

108. Type 2 Antidiabetic drugs
• Sulphonylureas
– Glibenclamide (Daonil)
Side effects
– Glicazide (Daimicron) • Hypoglycaemia: fatigue,
– Glimepiride (Amaryl) tremors, hunger, headache,
– Glipizide (Glibenese)
Actions
palpitations, blurred vision,
– Act on the pancreas and block ATP confusion, cold sweats,
potassium channels which causes influx of convulsions, coma
calcium and insulin release. Also reduce
glucagon levels and stimulate binding of • Weight gain
insulin to target tissues.
• Glucosidase inhibitors • HyperInsulinemia
– Acarbose (Glucobay) • Acarbose and Metformin –
• Biguanides
– Metformin (Glucophage)
GI disturbances: flatulence,
Actions diarrhoea, cramping. Rarely
– Inhibits glucogenesis in the liver reducing lactic acidosis
the output of glucose from the Liver and
blood sugar levels

109. Anti-diabetic drugs

110. Antibacterial –Nucleic acid inhibition
• Sulphonamides (UTI) Side effects
– Nitrofurantoin (Furandantin, Macrobid)
– Trimethoprim (pneumocystis carinii) • nephrotoxicity due to crystalluria,
(Monotrim Suspension) • hypersensitivity reactions from
Actions
rash to angioedema.
– Prevents DNA synthesis
– Inhibits B5 (important in AA synthesis) • Serious blood reactions e.g.
Uses granulocytopenia,
• Respiratory Tract Infections thrombocytopenia, megaloblastic
• GI Tract Infections
anemia, leukopenia, haemolytic
• Urinary Tract Infections
• Genital Tract Infections
anemia.
– Sulphonamides (UTI) • Other side effects – nausea,
– Strep pneumoniae vomiting, stomach pain.
– Nocardia asteroide,
– H influenzae, • Contraindicated in pregnant
– E Coli, Shigella women and infants under 2
– Trimethoprim months
– Listeria monocytogenes, H Influenzae,
Legionella pneumonphillia, E Coli, Proteus
mirabilis, Salmonella typhi, Shigella

111. Antibacterial –Nucleic acid inhibition
• Quinolones Side effects
– Ciprofloxacin (Ciproxin,
Biofloxcin) • Diarrhoea/nausea,
– Levofloxacin (Tanavic) vomiting,
– Moxifloxacin (Avelox) • Headache/dizziness,
Actions phototoxicity.
– Prevents DNA synthesis
– Inhibits B5 (important in AA
• To be avoided in pregnancy
synthesis) and breast feeding and in
Uses children under 18.
– Neisseria gonorrhoeae, Bacillus • Can cause articular cartilage
anthracis, Enterobacteriaceae, E Coli,
Psuedomonas, Klebsiella erosion, causing ruptured
pneumoniae, Proteus mirabilis, tendons in adulthood.
Serratia marcescens, Shigella, H
Influenzae, Legionella pneumophillia
(Legionnaires Disease), Mycoplasma
pneumonia, Chlamydia pneumonia,
Mycobacterium tuberculosis

112. Antibacterial –Nucleic acid inhibition
• 5-Nitroimidazoles Side effects
– Metronidazole (anaeobic infn.) • Dapsone – methemoglobinemia,
(Flagyl, Metronide) peripheral neuropathy, erythema
– Rifampicin (TB, Leprosy) (Rifadin) nodosum
Actions • Ethambutol – optic nerve neuritis,
– Prevents cell walls formation and inhibits decrease in vision, colour blindness,
protein folate and RNA synthesis. worsens gout
Uses • Isoniazid – hypersensitivity reactions,
peripheral neuritis, paresthesias,
– Mycobacterial infections: convulsions in patients prone to seizures,
– TB mental abnormalities, optic nerve neuritis
– Leprosy • Rifampicin – nausea and vomiting, fever,
– Pneumocystis rash, jaundice. Caution in patients with
– Neisseria Meningitidis, chronic liver disease, alcoholics and the
– H Influenzae elderly
– Lung Infections • Rifabutin – rash, neutropenia, liver
function text abnormalities, anemia,
– Genitourinary Tract Infections thrombocytopenia
– Meningitis • Pyrazinamide – gout, nausea, hepatitis,
hyperuricemia, rash, joint pain

113. Antibacterial – nucleic acid inhibition

114. Antibacterial – cell wall inhibition
• Penicillins • Cephalosporins
– Benzylpenicillin (Crystapen) • Orally active
– Penicillin V (Calvepen) – Cefaclor (RTI, otitis media,
• Broad spectrum soft tissue, UTI,
– Amoxicillin (RTI, GU, gynae, nasopharyngeal) (Distaclor,
gonorrhoea, peritonitis, bac endocardiitis, Keftid)
septicaemia, wound infn)(Augmentin, – Cefuroxime (Zinacef)
Amoxil) – Cephalexin (RTI, otitis media,
– Ampicillin (septicaemia, endocarditis, soft tissue, GU, dental infn)
osteomyelitis, meningitis, abdominal (Keflex)
surgery)(Penbritin, Clonamp)
– Ceftriaxone (RTI, Renal, UTI,
• Penicillinase resistant septicaemia, meningitis, soft
– Flucloxacillin (staph infn., tissue, gonorrhoea) (Rosephin)
endocarditis) (Flucillin) • Vancomycin (staph enterocolitis)
• Antipseudomonal (Vancocin Matrigel)
– Piperacillin, Tazobactam (RTI, • Teicoplanin (staph inf prophylactic)
intra-abdominal, septicaemia, (Targocid)
neutropenia) (Tazocin)

115. Antibacterial – cell wall inhibition
Side Effects
• Diarrhoea
• Nausea and Vomiting
• Abdominal Pain
• Swollen Tongue
• Bruising
• Jaundice
• Rash
• Itching
• Fever
• Sore Throat
• Nephritis
• Neurotoxicity - especially in Epileptic patients
• Eosinophilia

116. Antibacterial – cell wall inhibition

117. Antibacterial – protein synthesis inhibition
• Actions • Chloramphenicol (eye infn) (Chloromycetin)
• Attack bacterial ribosomes, prevents protein • Macrolides
synthesis – Clarythromycin (RTI, acute otitis media, H.Pylori, ST infn)
• Tetracyclines (Klacid)
– Doxycycline (RTI, sinusitis, UTI, STI, cholera, plague) – Erythromycin (Erythroped, Erythyrocin)
(Vibramycin) – Azithromycin (RTI, otitis media, genital chlamidia infn)
– Minocycline (acne) (Minosil) (Zithromax, Azromax)
– Uses – Uses
– Bacillus antracis – Staph aureus/pneumoniae/pyogenes
– Brucella – Corynebacterium diphtheriae
– Vibrio cholerae – Bordetella pertussis
– Yersinia pestis – Capmyobacter jejuni
– Clostridium perfingens – Treponema palladium
• Aminoglycosides • Others
– Amikacin (pseudomonal infn) (Amikin) – Dalfopristin, Quinpristin (Serious gram+ infn)
(Synercid)
– Tobramysin (chronic airways infn pseudomonas)
(Cidomycin, Genticin)
– Gentamicin
• Uses
– Enterococcus Gram +ve
– Brucella
– Klebsiella
– Pseudomonas
– Yersinia Pestis

118. Antibacterial – protein synthesis inhibition

119. Antifungal drugs
Antifungal – Side effects
• Polyenes – Nausea, vomiting, skin irritation, H/A
– Amphotericin B (Aspergilliosis, candida, • Clotrimazole – skin burns
cryptococcal meningitis, histoplamosis) (Albecet) • Fluconazole – abdominal distension,
– Nystatin (Candida) (Mycostatin) diarrhoea, hepatitis
• Imidazoles[Topical] • Flucytosine – neutropenia,
– Clotrimazole (Candida) (Canestan) thrombocytopenia, bone marrow
depression, alters liver function tests, severe
– Ketoconazole (candida) (Nizoral) enterocolitis
• Triazoles • Itraconazole – hypokalemia, hypertension,
– Fluconazole (candida, meningitis) (Diflucan, oedema
Byfluc, Diflazole) • Ketoconzole –abdominal pain, gynecomastia,
– Itraconazole (Candida, histoplasmosis, decreased libido, impotence, menstrual
cryptococcal infn) (Sporanox) problems, affects liver function tests,
• Flucytosine (Candida, crytococcal) (Ancotil) jaundice
• Terbinafine (histoplasmosis, cryptococcal [not • Miconazole – vaginal irritation
meningitis], systemic fungal) (Lamasil,
Fungafine) • Amphotericin –fever, bleeding symptoms,
• Caspofungin (candida, aspergillus) (Cancidas) abdominal pain, muscle and joint pain
• Nystatin – diarrhoea
• Terbinafine – blurred vision, affects liver
function tests, neutropenia, hepatotoxicity

120. Antiviral drugs
• Penetration inhibitors • Side effects
– Amantadine (flu prophylactic) • Acyclovir – headache, diarrhoea, nausea
(Symmetrel) and vomiting, renal dysfunction (high
• Nucleoside Reverse Transcriptase dose)
Inhibitors (NTRI’s) • Famiclovir – headaches, nausea,
– Stavudine (HIV) (Zerit) adenocarcinomas and testicular toxicity
– Zidovudine (HIV) (Retrovir) • Ganciclovir/Valganciclovir – GI upset,
– Tenofovir (HIV) (Viread) neutropenia, carcinogenic, embryotoxic
• Non-Nucleoside Reverse Transcriptase • Indinavir – headache, GI upset,
Inhibitors NNRI’s nephrolithiasis, hyperbilirubinemia
– Nevirapine (HIV) (Viramune) • Lamivudine – headache and dizziness
• Protease inhibitors • Oseltamivir – GI upset
– Ritonavir (HIV) Kaletra) • Ribaviran – elevated bilirubin, transient
anemia
– Saquinavir (HIV) (Invarase)
• Rimantidine – GI upset
• Neuramanidase inhibitor
• Valacyclovir – GI upset, thrombocytopenia
– Zanamivir (flu) (Relenza) purpura
• Herpes Simplex • Zanamivir – headache, sore throat, cough,
– Aciclovir (Zovirax) wheezing
– Famciclovir (recurrent genital herpes)
(Famvir)

121. Antifungal and antiviral drugs

122. Drugs – parasites - helminths
• Intestinal nematodes • Platyheminths
• Roundworm
– Piperazine, levamisole, mebendazole,
• Trematodes
• Hookworm – Schistosomiasis
– Bephenium, Trichlorethylene, Thiabendazole • Praziquantel
• Whipworm
– Mebendazole, thiabendazole – Cestodes
• Threadworm (common in children) • Praziquantel
– Thiabendazole, • Niclosamide
– Medendazole (GIT worms) • Side effects
(Vermox) • Albendazole – headache, nausea, liver toxicity,
agranulocytosis, pancytopenia
• Tissue Nematodes • Dying parasites can cause inflammatory
– Filaria (blood worms, if in lymphatics responses, headache, vomiting, fever,
convulsions and mental changes.
can cause obstruction and swelling) • Mebendazole – abdominal pain and diarrhoea
• Diethylcarbamazine • Ivermectin - fever, headache, dizziness,
somnolence and hypotension.
• Praziquantel – drowsiness, dizziness, malaise, GI
disturbance and poor appetite
• Thiabendazole – dizziness, poor appetite,
nausea, vomiting, erythema multiforme,
Stevens-Johnson syndrome (fever, skin lesions,
mucous membrane ulcers)

123. Drugs – parasites - helminths

124. Drugs parasites - protozoa
• Malaria (Plasmodium) • Amoebic dysentery
– Tissue schizonticide – Metronidazole (Flagyl)
• Primaquine • Giardiasis
– Blood schizonticide (If – Metronidazole (Flagyl)
clinical attack)
• Proguanil (Paludrine) • Trochonomiasis
• Mefloquine (Larium) – Metronidazole (Flagyl)
• Chloquine (Avloclor) • Pneumocytosis
– Pentamidine (Pentacarinat)
• Leishmanisasis
– Stibogluconate
(Pentostam)
• Tripanosomiasis
– Suramin (Germanin)

125. Drugs parasites - protozoa
• Amoebiasis (Amoebic Dysentery) • Chloroquine – nausea, diarrhoea,
(Metronidazole, Paromomycin, abdominal pain, headache, dizziness,
Tinidazole) hearing disorders, mood changes (see
Mefloquine), rash, blurred vision
• Cryptosporidiosis (Paromomycin)
• Doxyclycline – nausea, vomiting,
• Malaria (Chloroquine, Doxycycline, diarrhoea, mouth ulcers, headache, rash,
Mefloquine, Quinine, Quinidine, photosensitivity, blurred vision
Primaquine, Proguanil, • Mefloquine – nausea, vomiting, headache,
Pyrimethamine) dizziness, abdominal pain, depression,
• Giardiasis (Metronidazole, Tinidazole) anxiety, panic attacks, hallucinations,
delusions, hearing disorders
• Pneumocystis Pneumonia
• Primaquine – abdominal bloating,
(Atovaquone, Pentamidine, diarrhoea, methemoglobinemia,
Sulfonamides) granulocytopenia, agranulocytosis,
• Toxoplasmosis (Atovaquone, hemolytic anemia
Pyrimethamine, Sulfonamides) • Quinine – nausea, vomiting, diarrhoea,
• Trichomoniasis (Metronidazole, headache, tinnitus, dizziness, rash,
hearing loss, blurred vision
Tinidazole)
• Malarial Drugs – discoloration of mucous
• Trypanosomiasis (Sleeping sickness) membranes and nail beds, angina,
(Pentamidine, Primaquine) palpitations, arrhythmias

126. Drugs parasites - protozoa

127. Drugs used in cancer
Inhibit DNA synthesis Side effects
– Cytarabine (inhibits DNA • Nausea
polymerase)
• Antimetabolites • Vomiting
– Methotrexate • heart arrhythmias
• lymphocytic leukaemia, • Neutropenia
choriocarcinoma, Burkitt's
lymphoma, breast • Hair loss
– Capecitabine (Xeloda)
• colorectalcancer and breast cancer
– Fluorouracil
– Raltitrexed
– Mercaptopurine
– lymphocytic leukemia
• Vinca alkaloids -antimicrotubule
– Vinblastine
– Hodgkin’s lymphoma, cancer of
lung/breast/testicles, head and neck
– Vincristine
– Non-Hodgkin’s lymphoma,
lymphoblastic leukaemia,
• Taxanes
– Paclitaxel

128. Drugs used in cancer
Inactivate DNA • Alkylating agents are
• Alkylating agents carcinogenic and can cause
– Chlorambucil (Endoxana)
treatment induced
– multiple myeloma and
lymphocytic leukemia neoplasms many years after
– Ifosfamide (Mitozana) treatment
– Estramustine - prostate cancer • Common:
– Cyclophosphamide (Endoxana)
• Vomiting
– Burkitts lymphoma, breast
cancer • Stomatitis
– Melphalan (Alkaran) • poor appetite, diarrhoea
– multiple myeloma and
lymphocytic leukaemia • hair loss
– Bulsulfan (Busulfex, Myleran) • bone marrow suppression
– Granulocytic leukaemia

129. Drugs used in cancer
• Antibiotics (cytotoxics) Side effects
– Doxorubicin
– Hodgkin’s lymphoma, lung,
• Nausea
breast, bladder, stomach,
thyroid and uterine cancer,
• Vomiting
Kaposi’s sarcoma
• heart arrhythmias
– Actinomycin D (inhibits
transcription) • Neutropenia
– gestational trophoblastic
neoplasia, Wilms' tumour and • Hair loss
rhabdomyosarcoma
• Steroid hormones
– Glucocorticoids
– Oestrogens
– Anti-oestrogens
– Androgens
• Monoclonal antibodies
– Rituximab (B-Cell lymphoma)
(Mabthera)

130. Drugs used in cancer

131. Adverse drug reactions