Pharmacology Pure and Simple

Week 1 Hypertension
Calcium Channel Blockers:
Verapamil, Nifedepine, Amlodipine
Blocks L-type Ca2+ channels in T-tubules reduced Ca2+ into
myocyte and reduced mechanical activation of Ca2+ release
channels in SR reduced myocyte contraction
Arterial VSM vasodilation reduce BP
Heart reduce HR and contractility
Verapamil: higher affinity for heart
Nifedipine: higher affinity for VSM
SE: heart failure, hypotension, peripheral oedema, constipation
Potassium Channel Opener:
Minoxidil, Pinacidil

Opens potassium channels in VSM hyperpolarisation

relaxation - vasodilation
Minoxidil: Promotes hair growth more oxygen to hair follicle
treats alopecia.
Pinacidil: Reduces blood pressure.
SE: hypertrichosis (excessive hair growth), tachycardia, angina.
Beta Blockers:
Atenolol, Propranolol
Atenolol: Selective beta-1 blocker blocks beta-1 receptors on
heart reduces cardiac output.
SE: Bronchoconstriction (high dose blocks beta-2 as well),
inhibits glycogenolysis (fatigue).
Propranolol: Non-selective beta blocker blocks beta-1 and
beta-2 reduces cardiac output.
SE: Bronchoconstriction, nightmares, depression, reduced
glycogenolysis (fatigue)
Alpha Blockers:
Prazosin

Alpha-1 blocker relaxes VSM reduces peripheral resistance.

 SE: orthostatic hypotension, syncope, and nasal congestion.

Mixed Alpha/Beta Blocker:
Labetolol

Selective alpha-1 + non-selective beta-1 and beta-2 blocker

treats pregnancy induced pre-eclampsia.
SE: orthostatic hypotension, abrupt withdrawal = arrhythmia, preeclampsia.

ACE Inhibitors:
Lisinopril, Captopril, Enalapril

Inhibits ACE prevents Angiotensin II formation reduces

vasoconstriction & aldosterone secretion reduces peripheral
resistance and blood volume.
SE: Cough (inhibits bradykinin breakdown), first dose
hypotension.
Interacts with potassium sparing diuretics HYPERKALEMIA.

Thiazide Diuretics:
Hydrochlorothiazides

Inhibits NaCl co-transporter in the distal tubule reduces

sodium reabsorption increases sodium/potassium/chloride
excretion reduce blood volume reduce blood pressure.
Black people respond better to thiazides.
SE: hypokalemia, hyperuricemia (gout), metabolic alkalosis.

Potassium Sparing Diuretics:

Spironolactone, Eplerenone, Amiloride, Triamterene

Spironolactone & Eplerenone: Block aldosterone receptor

increase sodium excretion & decrease potassium excretion
reduces blood volume reduces BP
SE: hyperkalemia, gynecomastia, impotence.

Amiloride & Triamterene: Block sodium channel in distal

tubule and collecting duct inhibits sodium reabsorption and
potassium excretion reduce blood volume.
SE: hyperkalemia, heart palpitations, dry mouth, nausea/vomiting.

Loop Diuretics:
Furosemide

Inhibits Na/K/2Cl co-transporter in TAL of loop of henle

blocks NaCl reabsorption reduces blood volume.
SE: metabolic alkalosis, hypokalemia, hyperuricemia,
hypomagnesemia

Angiotensin II inhibitors:
Losartan, Valsartan
Block AII receptors - on VSM and adrenal cortex (blocks
aldosterone release).
Renin inhibitors:
Aliskiren
Blocks renin prevents activation of renin angiotensin aldosterone
system

LIPID LOWERING DRUGS:

Statins:
Atorvastatin, Fluvastatin
Inhibit HMG-CoA reductase inhibit cholesterol synthesis in
liver stimulate increase in LDL receptors on hepatocytes
increase LDL uptake in liver increase LDL catabolism reduce
plasma cholesterol reduce atherosclerosis
Also, decrease triglycerides + increases plasma HDL +
maintain plaque stability
PREGNANCY IS CONTRAINDICATED cholesterol essential for
foetal growth
SE: myositis, rhabdomyolysis (may cause acute renal failure),
headache (common)
Fibrates:
Gemfibrozil
Stimulates PPAR-alpha receptor increases lipoprotein lipase
synthesis stimulates hydroxylation of triglycerides to fatty
acids fatty acids are used by muscle (energy) and adipocytes
(storage)
Also, increased plasma HDL + reduced VLDL & LDL
SE: myositis
Bile Acid Sequestrants (Resin):
Cholestyramine

Liver uses cholesterol to produce bile acids - sequestrants

adsorbs bile acids -reduces GI absorption + increased
cholesterol excretion - reduced plasma cholesterol stimulates the liver to produce more bile acids - uses more
cholesterol further drop in cholesterol reduced atherosclerosis
SE: GI disorders

Week 2 - Heart Failure

Anticoagulants:
Heparin / LMWH

Binds Antithrombin III increases its activity by 1000-fold

inactivates Factor Xa + thrombin reduced clot formation.
LMWH only inactivates Factor Xa, it also has a longer half life.
Used for: VTE, PE, atrial fibrillation, HF.
SE: haemorrhage, thrombocytopenia (reduced platelets).

Warfarin

Inhibits vitamin K epoxide reductase prevents vitamin K

dependant carboxylation of glutamate residues of Factor II, VII, IX
and X.
Used for: same as heparin & prosthetic heart valve
thromboembolism.
Monitored with INR (prothrombin time) usually 2 to 3.
SE: haemorrhage, teratogen, abnormal bone development.

Cardiac Stimulant:
Digoxin

Digitalis glycoside inhibits Na/K pump increases

intracellular sodium slows the extrusion of calcium via
Na/Ca exchange transporter increases intracellular calcium
increases contractility of heart slows atrioventricular

conduction increases atrioventricular period decreases heart

rate.
Used for: A fib, heart failure.
SE: arrythmias, yellow/blurred vision, nausea/vomiting.

Week 3 Rheumatic Heart Disease

Anti-muscarinic:
Atropine

Blocks binding of ACh to muscarinic receptors blocks

parasympathetic (vagal) activity increases heart rate.
Given as a treatment for SLUDGE
(salivation, lacrimation, urination, diaphoresis, gastrointestinal motili
ty, emesis)
Prevents bradycardia during surgery, used as mydriatic, for
incontinence.
SE: tachycardia, mydriasis (pupil dilation), delirium, dry mouth,
constipation.

Beta-Lactams:
Penicillin
Amoxicillin + Clavulonate (Augmentin)
Amoxicillin: Inhibits cross-linking of cell wall peptidoglycans
preventing formation of bacterial cell wall + Clavulonic acid:
Inhibits beta lactamase
streptococci (RHD Group A), pneumococci, meningococci, syphilis
Penicillin V (Phenoxymethylpenicillin) - tonsillitis, pharyngitis,
rheumatic fever, skin infections
Penicillin G (Benzylpenicillin) - pneumonia (community
acquired), endocarditis, gonnorrhea, cellulitis, meningitis - more
active against Gram Negative

SE: GI problems, allergic reactions (rashes, anaphylactic

shock, seizures), diarrhoea, super infection.

Cephalosporins
Cefuroxime
Inhibits cross-linking of cell wall peptidoglycans preventing
formation of bacterial cell wall
Resistant to many beta-lactamases
Work better than penicillins on many gram negatives
Gram Negative: enterobacter, citrobacter
SE: GI problems, rash, diarrhoea, super infection

Week 4 Asthma
RELIEVERS:
Beta Agonists:
Short acting - Salbutamol (Albuterol), Terbutaline
Long acting - Salmeterol, Formoterol

Activates Beta-2 receptors in bronchial SM increases cAMP

activates protein kinase A inhibits myosin phosphorylation
muscle relaxation bronchodilation.
Also - increases cilia beating & blocks vagal impulses
(decrease SM constriction).
SE: tachycardia, muscle tremor, restlessness.

Methylxanthines:
Theophylline, Aminophylline

Inhibits phosphorylation of phosphodiesterases prevents

conversion of cAMP to AMP increase in cAMP - activates protein
kinase A inhibits myosin phosphorylation muscle relaxation
bronchodilation.
Also activates histone deacetylase downregulates
expression of pro-inflammatory genes reduced T cell
proliferation and cytokine production.

SE: tachycardia, nausea/vomiting, insomnia.

Anti-Muscarinic:
Ipratropium, Tiotropium

Blocks muscarinic receptors in bronchial SM & reduces

histamine stimulation of bronchial vagal afferents - prevents
vagal stimulated bronchoconstriction bronchodilation.
SE: cough, nasal dryness.

PREVENTERS:
Corticosteroids:
Beclamethasone (inhalation), Prednisolone (oral)

Diffuses into cells binds cytoplasmic glucocorticoid receptor

activated glucocorticoid receptor complex enters nucleus binds
steroid response element on DNA activates histone
deacetylases - represses genes by inhibiting pro-inflammatory
transcription factors (eg. NFkB) reduces eosinophil
infiltration, inhibits macrophage function, reduces vascular
permeability, reduces leukotrienes.
SE: oral candidiasis & dysphonia (inhaled); infections, muscle
wasting, osteoporosis, psychosis, diabetes, hypertension,
hypokalemia, skin atrophy, poor wound healing, growth
suppression in children, Cushingoid appearance (moon face,
buffalo hump).

Leukotriene receptor antagonists:

Montelukast, Zafirlukast

Blocks cysteinyl leukotriene-1 receptor for leukotrienes LTC4,

LTD4, LTE4 prevents bronchconstriction, mucous
hypersecretion, airway inflammation, oedema.
SE: none are common.

Leukotriene synthesis inhibitor:

Zileuton

Inhibits 5-lipoxygenase inhibits leukotriene synthesis

prevents bronchconstriction, mucous hypersecretion, airway
inflammation, oedema.
SE: hepatitis (increased aminotransferase levels), flu-like syndrome,
dyspepsia.

Mast Cell Stabilisers:

Cromolyn, Nedocromil

Blocks calcium entry into mast cells and basophils prevents

release of histamine, leukotrienes, other mediators.
SE: nasal and throat irritation.

IgE antagonist:
Omalizumab

Binds to IgE antibody prevents binding of IgE to mast cells

and basophils blocks release of histamine and leukotrienes.
SE: anaphylaxis (severe allergic reaction).

ASTHMA DIAGNOSIS:
Challenge Tests - Bronchoconstrictors
Methacholine - muscarinic agonist- imitates acetylcholine- used to
diagnose asthma
Histamine - stimulates vagal afferents

Week 7 Glaucoma
AQUEOUS HUMOR SECRETION:
Carbonic Anhydrase Inhibitor:
Acetazolamide, Dorzolamide
Acts on ciliary body epithelium in the posterior chamber of eye
inhibits carbonic anhydrase - inhibits bicarbonate synthesis
reduces sodium transport (bicarb / sodium co-transporter)
reduced aqueous formation reduced intraocular pressure.
Used for: open angle glaucoma.
SE: diuresis, parasthesia (tingling), kidney stones.
Beta-blockers:
Timolol, Betaxolol, Carteolol
Blocks beta-2 adrenoceptors in the ciliary body epithelium
reduces aqueous formation reduced intraocular pressure.
SE: bronchospasm (asthmatics), bradycardia, heart failure.

 AQUEOUS HUMOR OUTFLOW:

Prostaglandin-F2 analogues:
Latanoprost
Passes through cornea binding prostaglandin FP receptor activates matrix metalloproteinases reduces outflow
resistance increases aqueous outflow through trabecular
meshwork into canal of schlemm reduce IOP.
SE: permanently alters iris colour (increases melanin in
melanocytes).
Muscarinic Receptor Agonist:
Pilocarpine, Carbachol
Activates muscarinic receptor in ciliary muscle contracts
ciliary muscle stretches trabecular meshwork increases
aqueous humor outflow reduce IOP.
SE: myosis (pupillary constriction), blurred vision.
Cholinesterase inhibitor:
Physostigmine
Inhibits cholinesterase decrease breakdown of ACh increase
stimulation of ciliary muscle muscarinic receptors contracts ciliary
muscle same as above.
SE: cholinergic syndrome (overdose), nausea/vomiting.
MACULAR DEGENERATION:
VEGF inhibitors:
Ranibizumab, Pegaptanib

Binds to and inhibits VEGF-A reduces choroidal

neovascularisation alleviates macular degeneration.
SE: conjunctival hemorrhage, eye pain, vitreous floaters,
increased intraocular pressure, and intraocular inflammation.

Week 8 Epilepsy
Sodium Channel Blockers:
Phenytoin, Carbamazapine, Lamotrigine

Blocks voltage gated Na+ channels preferentially blocks cells

firing with high frequency prevents release of glutamate
prevents spread of seizure.
Used for: partial seizures, generalised tonic clonic seizures,
status epilepticus (after IV diazepam), trigeminal neuralgia,
bipolar
SE: ataxia, diplopia, nystagmus, photosensitivity.

Sodium Channel Blockers / GABA augmenter / Calcium Channel

Blocker:
Valproate, Ethosuximide

Blocks voltage gated Na+ channels; Increases GABA by

increasing release / decreasing metabolism / reducing
reuptake; Blocks T-type calcium channels blocks 3/sec
firing rhythm in thalamic neurons (characteristic of absence
seizures)
Used for: absence seizures, complex partial seizures, tonic clonic,
myoclonic, migraines, bipolar.
SE: GI problems, dizziness, hepatotoxicity, sedation, teratogen

Sodium Channel Blockers / GABA augmenter / Glutamate Receptor

Blocker:
Topiramate

Blocks voltage gated Na+ channels; Increases stimulation of

GABAA receptors; Blocks glutamate (AMPA) receptor.
Used for: partial seizures, tonic clonic seizures.
SE: ataxia, fatigue, impaired concentration & memory, speech
problems, diplopia.

Barbiturates:
Phenobarbital

Stimulates GABAA chloride channels increases duration of

chloride ion channel opening; Also inhibits glutamate activation
at the AMPA receptor.
Used for: febrile seizures in children.
SE: delirium, dependence, hangover, lethargy.

Benzodiazapenes:
Short acting - Midazolam, Alprazolam, Lorazepam, Clonazepam
Long acting - Diazepam, Chlordiazepoxide (Librium)

Stimulates GABAA chloride channels increases frequency of

chloride ion channel opening.
Sedative, hypnotic, anxiolytic, anticonvulsant, muscle relaxant,
amnesic.
Used for: Anxiety, alcohol withdrawal (chlordiazepoxide), preop sedation (lorazepam), status epilepticus (diazepam),
muscle spasm

SE: dependence (short acting), drowsiness, amnesia, respiratory

depression.
Withdrawals: anxiety, insomnia, irritability, depressed mood.
Overdose: Flumazenil competitive inhibitor of the benzo
binding site on GABAA.

Others:
Gabapentin, Pregabalin: GABA analog - does not act on GABA
receptor may stop expression of Ca2+ channels
Felbamate: Blocks NMDA receptors
Z-drugs: Zolpidem, Zopiclone: Non-benzodiazepine hypnotics.
Binds GABAA at same location as benzos. Less dependence + better
sleep (lose less REM sleep).

Week 9 Multiple Sclerosis

Benzodiazapenes:
Short acting - Midazolam, Alprazolam, Lorazepam, Clonazepam
Long acting - Diazepam, Chlordiazepoxide (Librium)

Stimulates GABAA chloride channels increases frequency of

chloride ion channel opening.
Sedative, hypnotic, anxiolytic, anticonvulsant, muscle relaxant,
amnesic.
Used for: Anxiety, alcohol withdrawal (chlordiazepoxide), preop sedation (lorazepam), status epilepticus (diazepam),
muscle spasm
SE: dependence (short acting), drowsiness, amnesia, respiratory
depression.
Withdrawals: anxiety, insomnia, irritability, depressed mood.
Overdose: Flumazenil competitive inhibitor of the benzo
binding site on GABAA.

Anti-muscarinic:
Atropine

Blocks binding of ACh to muscarinic receptors blocks

parasympathetic (vagal) activity increases heart rate.
Given as a treatment for SLUDGE
(salivation, lacrimation, urination, diaphoresis, gastrointestinal motili
ty, emesis)
Prevents bradycardia during surgery, used as mydriatic, for
incontinence.
SE: tachycardia, mydriasis (pupil dilation), delirium, dry mouth,
constipation.

Anti-spastic:
Baclofen

Stimulates GABAB receptors reduces cAMP inhibits Ca2+

channel opening + increases K+ conductance- hyperpolarizes
cell muscle relaxation
Used for: Cerebral palsy, MS, Amyotrophic lateral sclerosis (Lou
Gehrigs disease), spasticity, tardive dykinesia.
SE: drowsiness, withdrawal.

Corticosteroids:

Beclamethasone (inhalation), Prednisolone (oral)

Diffuses into cells binds cytoplasmic glucocorticoid receptor

activated glucocorticoid receptor complex enters nucleus binds
steroid response element on DNA activates histone
deacetylases - represses genes by inhibiting pro-inflammatory
transcription factors (eg. NFkB) reduces eosinophil
infiltration, inhibits macrophage function, reduces vascular
permeability, reduces leukotrienes.
SE: oral candidiasis & dysphonia (inhaled); infections, muscle
wasting, osteoporosis, psychosis, diabetes, hypertension,
hypokalemia, skin atrophy, poor wound healing, growth
suppression in children, Cushingoid appearance (moon face,
buffalo hump).

Disease Modifying Drugs:

Interferon Beta-1a, Interferon Beta-1b
Binds to cell surface receptors - immunosuppressive effects Improves BBB integrity
Reduces symptoms in Relapsing / Remitting MS
SE: flu-like symptoms, neutropenia, GI problems.
Glatiramer Acetate

Random polymer that mimics myelin basic protein acts as

decoy from autoimmune response.
SE: flu-like symptoms, flushing, SOB, anxiety, rapid pulse.

Natalizumab

Interferes with Integrin receptor molecules reduces ability

of immune cells to cross BBB.
SE: progressive multi-focal leukoencephalopathy (when given
with IFN beta), arthralgia, headache.

Week 10 Schizophrenia
NMDA Antagonist Dissociative Anaesthesia
Ketamine, Phencyclidine (PCP)

Blocks glutamate NMDA receptors produces dissociative

anaesthesia (analgesia, immobility, amnesia)
Does not depress respiration or loss of consciousness
Used for minor surgery (eg. Oesophagoscopy)
SE: hallucinations, short term memory loss, delirium, hypertension

ANTIPSYCHOTICS FIRST GENERATION - TYPICAL

Phenothiazines:
Chlorpromazine, Thioridazine, Fluphenazine
Butyrophenone:
Haloperidol

Antagonises D2 receptors in mesolimbic area, NTS and basal

ganglia.
Blocks muscarinic receptors. Also blocks H1,
alpha-1, serotonin receptors.
SE:
D2 Extra pyramidal side effects (EPSE) tardive dyskenesia
(repetitive movements of face and neck), dystonia (muscle spasms
causing twisting and abnormal postures), akathesia (restlessness),
parkinsonism, neuroleptic malignant syndrome
Muscarinic - tachycardia, mydriasis (pupil dilation), delirium, dry
mouth, constipation
Alpha-1 low BP
Histamine sedation, antiemetic.
Serotonin anxiolytic, anti-aggressive, anti hallucinations

Chlorpromazine: High muscarinic. Lower EPSEs

 Thioridazine: Retinal pigmentation (melanosis)

Haloperidol: Lower muscarinic. High EPSEs
ANTIPSYCHOTICS SECOND GENERATION ATYPICAL
Atypical: Less EPSEs
Clozapine

Blocks D4 > D2 (Less EPSEs);Blocks M1-M5 (less EPSEs);

Blocks 5HT2a (anti hallucinations, less
EPSEs); Blocks 5HT2c (weight gain).
SE: AGRANULOCYTOSIS, plus all above.

Olanzapine, Risperidone

Blocks 5HT2 > D2; Blocks M1; Blocks H1

SE: weight gain, type 2 diabetes, orthostatic hypotension, plus all
above.

Week 11 Anxiety / Dementia

Acetylcholinesterase inhibitor:
Physostigmine, Donepezil, Galantamine

Inhibits acetylcholinesterase decrease breakdown of ACh

increase synaptic Ach slows decline of cognitive function.
Used for dementia, Alzheimers.
SE: cholinergic syndrome (overdose), GI problems, nausea/vomiting,
bradycardia.

Rivastigmine

Inhibits acetylcholinesterase and butrylcholinesterase

(decreased breakdown of succinylcholine) rest same as
above.
Metabolised at site of action no interactions.

Glutamate antagonist:
Memantine

Low affinity, non-competitive, NMDA receptor antagonist

prevents excitotoxic glutamate effects decreases neuronal
loss slows decline of cognitive function.
SE: confusion, insomnia, headache.

Anxiolytic:
Buspirone

Activates presynaptic 5HT1a (inhibitory neurotransmission)

in dorsal raphe nucleus decreases firing of serotonergic
neurons.
Used for: generalised anxiety disorder (GAD)
SE: headache, fatigue, blurred vision, sweating, tachycardia.

Barbiturates:
Phenobarbital

Stimulates GABAA chloride channels increases duration of

chloride ion channel opening; Also inhibits glutamate activation
at the AMPA receptor.
Used for: febrile seizures in children.
SE: delirium, dependence, hangover, lethargy.

Benzodiazapenes:
Short acting - Midazolam, Alprazolam, Lorazepam, Clonazepam
Long acting - Diazepam, Chlordiazepoxide

Stimulates GABAA Cl- channels increases frequency of Cl- ion

channel opening.
Sedative, hypnotic, anxiolytic, anticonvulsant, muscle relaxant,
amnesic.
Used for: Anxiety, alcohol withdrawal (chlordiazepoxide), preop sedation (lorazepam), status epilepticus (diazepam),
muscle spasm
SE: dependence (short acting), drowsiness, amnesia, respiratory
depression.
Withdrawals: anxiety, insomnia, irritability, depressed mood.
Overdose: Flumazenil competitive inhibitor of the benzo
binding site on GABAA.

SSRIs:
SSRI - Fluoxetine, Sertraline, Paroxetine

inhibit reuptake of 5HT after release into synapse improve

mood
SE: sexual dysfunction, suicidal ideation, apathy, withdrawals,
weight gain / loss

Week 12 Eating Disorder

Cannabinoid agonist:
Dronabinol

CB-1 rcp agonist increases appetite.

Used for anorexia
SE: short term memory

Cannabinoid antagonist:
Rimonabant

CB1 rcp antagonist suppresses appetite.

Used for anti-obesity, smoking cessation, blocks cannabis effects
SE: depression

Week 13 Acute Renal Failure

Beta Blockers:
Propranolol
Non-selective beta blocker blocks beta-1 and beta-2 reduces
cardiac output.
SE: Bronchoconstriction, nightmares, mood depression, inhibits
glycogenolysis (fatigue)

Nasal / Sinus Decongestant:

Pseudoephedrine

Alpha adrenergic receptor agonist & increases release of NA

vasoconstriction and cardiac stimulation.
SE: nervousness, tachycardia, insomnia, CNS stimulation.

Urologic Agent:
Terazosin

Selective alpha-1 receptor antagonist lowers BP decreases

outflow obstruction caused by an enlarged prostate.

SE: First dose syncope, priapism, erectile dysfunction.

Type 1 Renal Tubular Acidosis:

Lithium, Amphotericin B

Failure of H+ secretion by the kidneys.

Type 2 Renal Tubular Acidosis:

Acetazolamide

Failure of HCO3- reabsorption by the kidneys - carbonic

anhydrase inhibitor

Week 8 Pneumonia
PROTEIN SYNTHESIS INHIBITORS:
Macrolides
Erythromycin, Azithromycin, Clarithromycin
Binds to 50S subunit- - prevents peptidyltransferase adding
peptidyl to AAs - inhibits protein synthesis.
Bacteriostatic
Gram Positive: streptococcus pneumonia, pneumococci,
staphylococci, enterrococci.
Gram Negative: Chlamydia, haemophilus influenza, legionella
U + LRTIs (phanyngitis, pneumonia) + sinusitis, otitis media
SE: GI problems
Tetracyclines
Doxycycline

Bind to 30S subunit- prevents binding of aminoacyl-tRNA to

ribosome subunit inhibits protein synthesis.
Bacteriostatic
Gram Negative: Chlamydia, gonorrhoea, syphilis, Borrelia
burgdorferi (Lyme Disease) mycoplasma, Rickettsia,
STIs, acne, cholera
SE: permanent teeth discolouration, teratogen,
photosensitivity, GI problems

Aminoglycosides:

Gentamicin, Streptomycin

Binds 30s subunit misreading of genetic code inhibits protein

synthesis.
Bacteriocidal

DNA SYNTHESIS INHIBITORS:

Fluoroquinolones:
Ciprofloxacin

Inhibits bacterial DNA topoisomerase type 2 (DNA gyrase)

and type 4
prevents DNA replication
Bacteriocidal
CELL WALL INHIBITORS:
Beta-Lactams:
Penicillin
Amoxicillin + Clavulonate (Augmentin)
Amoxicillin: Inhibits cross-linking of cell wall peptidoglycans
preventing formation of bacterial cell wall + Clavulonic acid:
Inhibits beta lactamase
streptococci (RHD Group A), pneumococci, meningococci, syphilis
Penicillin V (Phenoxymethylpenicillin) - tonsillitis, pharyngitis,
rheumatic fever, skin infections
Penicillin G (Benzylpenicillin) - pneumonia (community
acquired), endocarditis, gonnorrhea, cellulitis, meningitis - more
active against Gram Negative
SE: GI problems, allergic reactions (rashes, anaphylactic
shock, seizures), diarrhoea, super infection.
Cephalosporins
Cefuroxime
Inhibits cross-linking of cell wall peptidoglycans preventing
formation of bacterial cell wall
Resistant to many beta-lactamases
Work better than penicillins on many gram negatives
Gram Negative: enterobacter, citrobacter
SE: GI problems, rash, diarrhoea, super infection.
Vancomycin

Binds to the D-alanyl-d-alanine portions of peptidoglycan prevents cross-linking of d-alanine and pentaglycine chain
prevents cell wall synthesis
Used for: MRSA (methicillin resistant staphylococcus aureus).

ANTI PROTAZOAL:
Nitroimadazole:
Metronidazole

Produces free radicals that attack DNA and proteins

Used for ANAEROBIC BACTERIA: Clostridium difficile,
trichomoniasis (vaginitis)

OTHERS:
Anti-Tuberculin:
Rifampicin
Inhibits RNA polymerase prevents transcription to RNA and
translation to proteins
Mycobacterium (eg. Tuberculosis) sometimes used as
prophylaxis for Neisseria meningitidis (meningococcal) infection
Sulfonamide:
Sulfadiazine
Inhibits folic acid synthesis blocks bacterial DNA synthesis
Used for: toxoplasmosis, UTIs

ANTI-BIOTIC RESISTANCE:
-

Betalactamase - breaks down B-lactam ring (gram-neg)

Plasmid- transfer of genetic info onto other bacteria

Penicillin binding proteins- change shape- cannot bind

Porins- conformation change- ABs cannot enter bacteria

Week 10 Multiple Myeloma

NSAIDs:
Aspirin (acetylsalicylic acid)

Adds acetyl group to COX irreversibly inhibits COX-1 prevents

conversion of arachadonic acid to PGH2 (analgesic, anti-pyretic,
anti-inflammatory effect) - therefore prevents thromboxane A2
and prostacyclin(PGI2) production prevents platelet
aggregation- also binds COX-2 (less preferentially)
SE: GI bleeding, heart burn, renal failure

Diclofenac, Ibuprofen

Non-selective, reversible COX inhibitor - prevents conversion of

arachadonic acid to PGH2 (analgesic, anti-pyretic, antiinflammatory effect).
SE: GI bleeding, heart burn, renal failure, priapism (ibuprofen)

Paracetamol

Selective COX-3 inhibitor - prevents conversion of arachadonic

acid to PGH2 (analgesic, anti-pyretic)
SE: Hepatic failure (overdose)

Overdose: Glutathione - conjugates to NAPQI and helps to

detoxify it - when normal pathway saturated (i.e. all glutathione
has been spent) , accumulated NAPQI reacts with hepatic
enzymes, killing hepatocytes - treatment for OD is N-Acetyl-LCysteine - augments glutathione reserves in body protects
hepatocytes from NAPQI

Opioids:
Codeine

CYP4502D6 catalyzes codeine to morphine- activates u opioid

receptorsopens K+ channels and closes Ca2+
channels- decreases release of SP and other NTs inhibits pain
neurotransmission in CNS
SE: respiratory depression, addiction

Local Anaesthetic:
Lidocaine, Procaine

Blocks voltage gated Na+ channels blocks nerve conductionreduced sensation

SE: dizziness, drowsiness, confusion
Chemotherapeutic Agent:
Vincristine

binds to tubulin dimers inhibits assembly of mitotic spindle

microtubules halts mitosis in metaphase prevents cell
division and tumour growth
SE: alopecia (hair loss), peripheral neuropathy, constipation,
hyponatremia

Cisplatin

Platinum compound - cross links DNA strands interferes with

mitosis
SE: nausea, vomiting (highly emetogenic use with ondansetron
- anti-emetic) nephrotoxicity, neurotoxicity

Methotrexate

Inhibits folate reductase prevents formation of folate stops

DNA base production halts mitosis in S phase

Used for cancer, RA, psoriasis

SE: teratogenic, ulcerative stomatitis (inflammation of mucous
lining of mouth), leukopenia, thrombocytopenia, anaemia

Week 12 Herpes Simplex Virus

Nucleoside Analogues:
Aciclovir, Ganciclovir

Nucleoside analogues incorporated into viral DNA - inhibits

viral DNA polymerase causes viral DNA chain termination
Used for: HSV-1 (trigeminal), HSV-2 (sacral root ganglion), VZV
(chicken pox),
EBV (glandular fever), CMV (salivary glands)
SE: dizziness, diarrhoea, nausea

Quick Drugs
Osteoporosis:
Etidronate: 1st generation bisphosphonate - binds to hydroxypatite
crystals in bones - reduces osteoclastic activity + decreased
activity of osteoblasts reduces bone resorption Alendronate and Risedronate: 2nd generation bisphosphonate binds
to hydroxypatite crystals in bones - reduces osteoclastic activity doesnt inhibit osteoblasts!
SE: Oesophagitis
Myasthenia Gravis:
Botulinum Toxin - cleaves SNARE proteins- blocks fusion of vesicles
with neuronal membrane- no release of ACh- blocks neuromuscular
transmission relieves spasticity
Dantrolene - inhibits ryanodine receptor- reduced intracellular
calcium from SR- relieves spasticity

Neostigmine - acetylcholinesterase inhibitor medium acting (1-2

hrs) SE: bradycardia
Edrophonium (Tensilon)- acetylcholinesterase inhibitor short
acting - (10mins)
COPD:
Varenicline- acts on nicotinic receptors in Ventral Tegmental Areablocks pleasurable effects of nicotine - also stimulates dopaminergic
neurons in nucleus accumbens- stimulates release of dopamineincreases risk of addiction
MI:
Clopidogrel- blocks platelet P2Y receptor- prevents stimulation by
ADP- prevent platelet aggregation
GTN- Glyceryl Trinitrate- forms nitric oxide- increased cGMPvasodilation SE: headache
Low dose - ven > art dilation- less venous return - decreased
contractility (Frank-Starling)
High dose - art > ven dilation- decreased TPR - decreased coronary
artery spasm
Sublingual
enters venous circulation (by-pass first pass)
faster and less risk of enzyme degradation- stomach and bile

IRDS:
Oxytocin- binds to oxytocin receptor- activation of phospholipase Cincreased intracellular Ca2+- activation of MLCK- UTERINE
CONTRACTION
TOCOLYTICS
Atosiban- oxytocin receptor blocker
Ritrodine, Terbutaline- beta 2 agonist- uterine muscle relaxation
(tocolytic)
Indometacin- COX inhibitor- no prostaglandins SE: renal
dysfunction, delayed closure of ductus arteriosus
Magnesium sulfate- blocks influx of Ca2+ into myometrial cells
GORD:

Cimetidine, Ranitidine, Famotidine (Zantac) - H2 receptor

antagonists- prevent activation of parietal cell H+/K+ ATPase
reduced acid secretion SE: Pernicous Anaemia (Megaloblastic) - due
to reduced release of intrinsic factor (needed for Vit B12 absorption
-folate regeneration) from parietal cells
Omeprazole, Lansoprazole proton pump inhibitors - irreversibly
inhibit H+/K+ ATPase proton pump in gastric parietal cells - no
reduction in release of Intrinsic factor
NB: converted to active form in acidic environment- antacids can
interfere
Misoprostal- synthetic prostaglandin E1 analogue- decreased acid,
increased mucus- labour induction and erectile dysfunction
Metoclopramide - antiemetic and gastroprokinetic- D2 antagonist +
H4 antagonist- increased tone of contractions and relaxes
sphincters- increased gastric emptying
Diabetes:
Glucagon (Alpha cells) - adenylyl cyclase- increased cAMPglycogenolysis + gluconeogensis injection to treat severe
hypoglycemia- Diabetic coma
Insulin (Beta cells)- GLUT 2 transporter- takes up glucose- increase
ATP- closes potassium channel- depolarizes Islet cells insulin
released
Sulfonylureas- acts on beta cells of pancreas- blocks ATP sensitive
K+ channels- depolarizes beta cell- Ca2+ influx- insulin release DM II
Metformin Biguanide - decreased glucose release from
hepatocytes + increased uptake of glucose into adipocytes &
muscle cells via GLUT4 DM II SE: lactic acidosis
Incretins- GLP (Glucagon-like peptide 1) and GIP (glucose dependent
insulinotropic polypeptide) - increase insulin secreted from beta cells
Rheumatoid Arthritis:
Leflunomide- inhibits pyrimidine synthesis in activated T cells
reduced inflammation

Sulfasalazine- converted to 5-aminosalicyclic acid by bacteria in

colon - 5-aminoalicyclic acid- free radical scavenger reduced
inflammation
Etanercept, Infliximab - TNF alpha antagonists prevent
upregulation of fibroblasts + osteoclasts which produce MMPs that
erode cartilage and bone
Anakinra - IL-1 antagonist- prevents upregulation of fibroblasts +
osteoclasts which produce MMPs that erode cartilage and bone
Methotrexate folic acid antagonist prevents DNA base synthesis
often used in combination with Etanercept
Rituximab- monoclonal antibody against CD20 (B lymphocytes)
Shoulder Dislocation:
Levobupivacaine interscalene block - peripheral nerve block of
brachial plexus between anterior & middle scalene
Cerebral Palsy:
Clonidine, Tizamidine - alpha 2 agonist- reduce tone
NB: Clonidine > BP (reduce CO & PVR), Tizamidine > muscle relaxant
(reduce spasms)
Parkinsons Disease:
Ropinirole, Bromocriptine D2, D3 agonist - inhibits indirect
pathway - decreased termination of movement
L-dopa, Carbidopa - precursor of dopamine - L-DOPA can cross BBB,
dopamine cant normally synthesized from L-tyrosine and converted
to dopamine in CNS by decarboxylase enzyme also converted in
PNS by same enzyme, therefore, carbidopa (PNS Decarboxylase
Inhibitor) used with L-Dopa as it can be active in the PNS but
cannot penetrate into the CNS allowing dopamine to form only in
CNS
Entacapone - inhibits COMT prevents conversion of L-DOPA to 3-omethyldopa which cannot cross BBB - like carbidopa, it can also be used
as adjunct to L-DOPA

Selegiline- inhibits MAO-B prevents breakdown of dopamine may

be used with L-dopa, however, there is an increased risk of an acute
hypertensive episode Headache / Migraine:
Carbamazepine, Phenytoin - Blocks voltage gated Na+ channels
preferentially blocks cells firing with high frequency prevents
release of glutamate prevents spread of seizure also treats
trigeminal neuralgia
Gabapentin - GABA analog - does not act on GABA receptor may stop
expression of Ca2+ channels can be used to treat trigeminal
neuralgia
Sumatriptan - tryptamine (anti-migraine) drug - activates 5HT1B/1D receptors causing intracranial vasoconstriction of large
arteries - also presynaptic inhibition trigeminal nerve acts in PNS
Almotriptan, Eletriptan, Rizatriptan - crosses BBB- act in CNS fewer side effects and longer duration of action - Prescribe with:
DOMPERIDONE
Domperidone (Motilium) - increases gastric motility - speed up the
passage of food through the stomach into the intestine, which
physically helps prevent vomiting and reduces feelings of sickness,
bloating and fullness (migraine causes gastric stasis - nausea)
Depression:
Neuronal death in both prefrontal cortex and limbic system
(hippocampus) - implicated in depression
ANTIDEPRESSANT DRUG THEORY - increased intracellular cAMP
activation of PKA activates CREB protein expression of BDNF
neurogenesis + decreased neuronal loss in prefrontal cortex and
limbic system (particularly hippocampus)
MAOI - Selegiline - MAO-B inhibitor high dose inhibits MAOA (antidepressent effect)
TCAs - Amitriptyline - block alpha 2 autoreceptor uptake of
serotonin and noradrenaline
SSRI - Fluoxetine, Sertraline, Paroxetine - inhibit reuptake of 5HT

after release into synapse

Bipolar - decreased NA - decreased MHPG in urine (NA metabolite)
Anxiety increased NA increased MHPG in urine associated with
unipolar depression
Suicide Victims - Brain and CSF - decreased 5-HIAA (metabolite of
Serotonin)
Dexamethasone suppression test - glucocorticoid - should suppress
CRH, ACTH - no effect -levels of hydrocortisone remain the same in blood
high cortisol in depression