Respiratory
Drug Classes
Drugs
Tuberculocidal
Anti-Tuberculosis Drugs
Mycolic Acid synthesis inhibitor
Spectrum of Activities

Kill extracellular bacteria

Weakens intracellular bacteria
Rifampicin

CYP450 Inducer in HAART, change with Rifabutin
Side Effects

Orange discoloration of body fluid
Bind to B subunit of RNA polymerase, inhibit mRNA synthesis
Spectrum of Activities

Kill
o
Extracellular bacteria
o
Intacellular organism
o
Spurters
Fatty Acid Synthase inhibitor
Spectrum of Activites

Weakly kill intracellular bacteria
Pyrazinamide
Side Effects

Hyperuriceamia
Streptomycin
Bind to 30S ribosomal subunit, inhibit protein synthesis
Spectrum of Activities

Kill only extracellular bacteria
Ethambutol
Arabinogalactan synthesis inhibitor
Beta2 Agonists
Binds to Beta 2 receptors, stimulate Adenylate Cyclase
Methylxantine – Theophylline
Phosphodiesterase III inhibitor
Antimuscarinic Agent – Ipratropium Bromide
Competitively blocked M3 receptor of bronchiol smooth
muscle cells, inhibit Phospholipase C
Inhibits Phospholipase A2 in which involve in the formation of
Arachidonic Acid
Side Effects

Ototoxic

Nephrotoxic
Tuberculostatic
Side Effects

Optic Neurittis
Contraindicated in very young children


Bronchodilators
Drugs for COPD
Salbutamol – rapid onset, short duration
Salmeterol – slow onset, long duration

Narrow Therapeutic Index
Toxic Effects

Fatal arrhythmias

Fatal convulsion
Corticosteroid
Antiinflammato
ry
Agents
Mucolytics
Mechanism of Action
Isoniazid

CYP450 Inhibitor

Metabolize through acetylation, highly genetic
polymorphism
Side Effects

Peripheral neuropathy – supply Vit B6

Hepatotoxic
1.
2.
3.
Prednisolone – oral
Hydrocortisone – IV
Beclamethasone – inhalation
Mast Cells Stabilizer – Cromone
Leukotriene Receptor Antagonis
Inhibits the release of inflammatory mediators from mast cells
Selectively block Cysteine Leukotriene (LT) receptor
Leukotriene Synthesis Inhibitor – Zileuton
Inhibits lypoxygenase enzyme which involves in the coversion
of Arachidonic acid to Leukotriene
Splitting the disulfide bond that links proteins in the mucus


Montelukast
Zafirlukast
N-acetylcysteine/ Ambroxol
Musculoskeletal
Drug Classes
NSAIDs
Drugs
Non-Selective
COX Inhibitor
Selective COX2
Inhibitor
Symptomatic
Relieve
Anti-Gout
AntiHyperuriceamic
Agents
DMARDs
Mechanism of Action
Aspirin

Displace Warfarin from Albumin
Contraindication

Relative C/I
o
Asthma

Absolute C/I
o
Gouty Arthritis
o
Children – Reye Syndrome
o
Pregnant
Irreversibly and non-selectively both COX1 and COX 2
Celecoxib
Side Effects

Cardiovascular side effects
Corticostreroid
Side Effects

Osteoporosis

Cushing syndrome
COX2 selective NSAIDs

Diclofenac sodium

Celecoxib

Indomethecin
Colchicine

Low Therapeutic Index
Side Effects

Intractable diarrhea
Allopurinol – overproducer

Interaction with Azathioprine (requires
Xanthine Oxidase for metabolism)
Uricosuric Agents – undersecretor

Probenecid

Sulfinpyrazone
Selective COX2 inhibitor
Methotrexate
Side Effects
1.
Mucosal toxicity
2.
Myelosuppression
3.
Hepatotoxicity
Sulfasalazine
Side Effects

Steven Johnson syndrome
Hydroxychloroquine

Contraindicated in G6PD deficiency
Leflunomide

CYP450 Inhibitor

TERATOGENIC
Biological Agents
TNF-a Antibodies
(Not DMARDs)

Humanized – Adalimumab

Chimeric – Infliximab
Soluble TNF-a Receptors – Etanercept
IL-1 Receptor Antagonist – Anakinra
Inhibits Phospholipase A2 in which involve in the formation of Arachidonic Acid
Selective COX2 inhibitor
↓leukocytes migration and release of inflammatory mediators by binding with
intracellular tubulin, inhibiting its polymerization
Xanthine Oxidase inhibitor
Uricosuric drugs act by affecting the active transports so that the net reabsorption of
uric acid will be ↓



Irreversible inhibition of Dihydrofolate reductase (DHFR)
Partially reversible inihibiton of Thymidylate synthetase
Inhibition of Aminoimidazolecarboxamide Ribonucleotide Transformylase
(AICAR)
Suppression of T cell and subsequently leading to ↓in B cells
Inhibits the release of inflammatory cytokines which are produced by
macrophages and monocytes
Uncertain


inhibit Dihydroorotate Dehydrogenase, an enzyme requires for synthesis of
ribonucleotide
Form complex with soluble TNF-a, therefore prevents its interaction with p55 and p75
receptors on various tissues
Binds with TNF-a therefore inhibiting it from binding to bound receptor
Competitively inhibiting the binding of IL-1 to the Interleukin-1 type receptor
Cardiovascular
Drugs
Drug Classes
Negative Inotropic,
Chronotropic and Dromotropic
Agents
Chronic Isheamic Heart
Disease Therapeutic
Intervention
Agents Reducing Afterload
Agents Reducing Afterload and
Preload
Anti-Ischeamic Metabolic
Agent
Antiplatelet
Mechanism of Action
Non-Selective Beta Blocker – Propanolol
Contraindication
 Asthma
 COPD
 Heart block
 Peripheral heart disease
Blocks both Beta 1 and Beta 2
receptors
If Channel Blocker – Ivabradine
Block the HCN channel/ Funny
channel
Blocks the Ca channel
 Inhibit the release of Ca and
leads to inhibition of
interaction between Myosin
and actin
 Inhibits muscle contraction
Calcium Channel Blocker
 Benzothiazepine
o Diltiazem – arteriole and heart
 Phenylalkylamine
o Verapamil – heart only
Contraindication
 Sinus bradycardia
 AV conduction defect
 Severe cardiac failure
Calcium Channel Blocker
 Dihydropyridine
o Nifedipine – arterioles only
Nitrates
 Glycyltrinitrate – sublingual
o For acute attack
 Isosorbide-5-mononitrate – oral
o For prophylaxis
Contraindication
 ICP
 Hypotension
 Severe hemolytic anemia
Drug interaction
 Viagra – severe hypotension
Nicotinamide Nitrate Ester – Nicorandil
Trimetazidine
Aspirin
Release Nitric Oxide, activating
Guanylylcylase
Develops tolerance quickly
Activate potassium channel
↑myocardial glucose utilization
through inhibition of fatty acid
metabolism
Nonselective COX inhibitor
Cardiovascular
Drugs
Drug Classes
Immediate
Treatment
Fibrinolytics and
Thrombolytic
Streptokinase – non-fibrin
specific
Alteplase – Fibrin specific
Aspirin
ADP Receptor Antagonist
 Ticlopidine – cause
Neutropenia
 Clopidogrel – not cause
Neutropenia
Acute Coronary
Syndrome Therapeutic
Intervention
Prophylaxis
Antiplatelet
Dipyridamole
Glycoprotein IIb/IIIa Platelet
Membrane Receptor Blocker
 Abciximab
Anti – Hyperlipideamic
Agents
Mechanism of Action
Streptokinase is given in order to bind to the
Plasminogen, which in return will allow Urokinase to
cleave Plasminogen into Plasmin. Then, protect the
Plasmin from being deactivated by plasma AntiPlasmin
Stimulates Plasminogen leading to clot dissolution
Nonselective COX inhibitor
non-competitive ADP receptor inhibitor
a. Inhibits platelete aggregation
b. ↓platelets conformational change
c. ↓release of platelet granules
d. ↓platelet amplification
1.
Inhibits Thromboxane Synthase
2.
Inhibits the reuptake of Adenosine
3.
Inhibits Phosphodiaesterase
Block receptor, stopping the common ligands from
activating the complex. This will therefore lead to
a.
Blocks formation of fibrin
b.
Inhibits platelet aggregation
HMG-CoA Reductase Inhibitor – Simvastatin
Side Effects
 Rhabdomyolisis
 Hepatotoxic
Vitamin B3 (Niacin) – Nicotinic Acid
Side Effects
 Hyperglyceamia
Inhibits HMG-CoA Reductase enzyme, use in
conversion of ACoA to Mevalonic Acid
ACoA  Mevalonic Acid  TG
Fibrates – Gemfibrozil
 Displace Warfarin from Albumin
Side Effects
 Rhabdomyolitis – if given with Statins
 Gallstone
 Hepatotoxic
Bile Acid Sequestrants – Cholestyramine

Intestinal Sterol Absorption Inhibitor – Ezetimibe
Magnifies the activity of Lipoprotein Lipase of
adipose tissues

Fibrate is a ligand of nuclear transcription
factor; PPAR-a
Stimulates Lipoprotein Lipase
Binds to bile acid in the gut, reduces bile acid
reabsorption as high as ten folds
Selective inhibitor of transport protein NPCL1L1,
important in the absorption of
a.
Cholesterol
b.
Phytosterols
Cardiovascular
Drug Classes
Drugs
Class 1
Sodium
Channel
Blockers
1.
2.
3.
Usage
1.
2.
Class 1b
 Lidocaine
1.
Low effect on blocking Na+ channel
2.
↑K+ conduction
3.
No effect on cardiac contractility
Usage
 Ventricular arrhythmias only
1.
The most potent Na+ channels blocker
2.
Does not have any activity on K+channel
3.
Some degree of beta receptors blockage
Usage
1.
Supraventricular arrhythmias
2.
Ventricular arrhythmias
Blocking the Beta receptor especially Beta 1 receptors on the
heart will inhibit the stimulation of sympathetic of the heart
Usage
1.
Supraventricular arrhythmias
2.
Ventricular arrhythmias
Pure Potassium channel blocker
1.
Blocks Na+ channels
2.
Blocks Beta adrenegic receptors
3.
Blocks K+ channels
4.
Blocks Ca2+ channels
Usage
1.
Supraventricular arrhythmias
2.
Ventricular arrhythmias
Class 1c
 Flecainide
 Propafenone
Antiarrhythmic Agents
Class 2
Beta Blockers
Class 3
Potassium
Channel
Blockers
Class 4
Calcium
Channel
Blocker
Mechanism of Action
Class 1a
 Qunidine
 Procainamide
Side Effects
 Cinchonism
Contraindication – Acute heary failure
 Displace Warfarin and Digoxin from Albumin
Beta Adrenergic Blocking Agent
 Propanolol
 Esmolol
 Metaprolol
Ibutilide
Amiodarone
 CYP450 Inhibitor
 Highly risk to get Torsades de Pointes
Side Effects
1.
Pulmonary fibrosis
2.
Impaired thyroid function
3.
Blue-grey discoloration of skin
4.
Impaired liver function
5.
Corneal micro-deposit
Calcium Channel Blocker
 Verapamil – heart
 Diltiazem – arteriole and heart
Blocks Na+ channels
Blocks K+ channels
Blocks Alpha receptors
Supraventricular arrhythmias
Ventricular arrhythmias
Blocks L type Ca2+ channels
Usage
 Supraventricular arrhythmias only
Haemopoetic and Lymphatic
Drugs
Drug Classes
Corticosteroid
Calcineurin Inhibitor
Interleukin Synthesis Inhibitor
Immunopharmacology
Immunosuppressive
Antiproliferative/Antimetabolite
Agents
mTOR (Mammalian
Target of Rapamycin)
Inhibitor
Mycophenolate Mofetil
Cyclopsporine
 CYP450 Inhibitor
and Inducer
Tacrolimus
Sirolimus/ Rapamune
Murine (Rat) Monoclonal Antibody
 Muromonab-CD3 (OKT3)
Immunosuppressive Antibodies
Thymoglobulin

Antithymocyte Globulin Rabbit
IL-2 Receptor Antibodies

Daclizumab – Humanized

Basiliximab – Chimeric
Cyclophospamide
Alkylating Agents
Folate Antagonist – Methotrexate
Anticancer Drugs
Antimetabolites
Pyrimidine Analogue – 5-Flurouracil
Purine Analogues
 Azathioprine – prodrug
 6-mercaptopurine – active metabolite
Plant Derivatives
Antitumour Antibiotics
Mechanism of Action
Inhibits Glucocorticoid Response Element (GRE) of
DNA.
Vinca Alkaloid

Vincristine – from Vinca rosea

Paclitaxel – from European yew
Doxorubicin
Side Effects

Cardiotoxicity
Binds to Immunophylin, the complex is then makes
Calcineurin to be dysfunctional
Binds to FKBP-12, the complex then makes the
Calcineurin to be dysfunctional
Sirolimus will binds to Immunophilin and this
Sirolimus-Immunophilin complex will inhibit the
mTOR actvitiy
Inhibits the Inosine Monophosphate (IMP)
Dehydrogenase enzyme
Muromonab will bind to CD3 protein on the T cells,
inhibiting lymphocyte function as access to
antigen recogition site is
Antibody binds to surface of the circulating T cells
Binds to IL-2 receptor alpha subunit on activated T
cell
Binds covalently with DNA, leading to

DNA fragmentation

Cross bridges formation

Mispairing of Nucleotides

Irreversible inhibition of Dihydrofolate
reductase (DHFR)

Partially reversible inihibiton of Thymidylate
synthetase

Inhibition of Aminoimidazolecarboxamide
Ribonucleotide

Inhibits Thymidylate Synthase

Inhibits RNA Polymerase
Inhibits enzymes involved in purine synthesis
Binds to tubulin and inhibits its polymerization
into microtubule
Interact with DNA by intercalation and
inhibition of macromolecular biosynthesis.
Haemopoetic and Lymphatic
Drugs
Drug Classes
Class 1
Asexual Erythrocytic stage
Antimalarial Drugs
Class 2
Primary Hepatic and
Eryhtrocytic Stage
Class 3
Primary and Secondary
Hepatic Stage
Mechanism of Action
Chloroquine
 Contraindicated in G6PD deficiency
 Long half life, use loading dose
 Resistance develops in P.falciparum
Inhibit the biocrytallization of heme into hemozoine
leading to build up of heme in the vacuole which toxic
to parasite
Spectrum of Activities
1. Highly effective blood schizonticide
2. Moderately effective against gametocytes
a. P. vivax
b. P.malariae
c. P.ovale
d. NOT P.falciparum
3. CANNOT against hepatic stage parasite
Quinine

Contraindicated in G6PD deficiency

Long half life, use loading dose
Side Effects

Quinine triads
o Cinchonism
o Hypoglyceamia
o Hypotension
Artemisnin Compound

Artesunate – water soluble

Artemether – lipid soluble

Dihydroartermisnin – water soluble
Folate Antagonist Combination
Fansidar

Pyrimethamine

Pyridoxine
Side Effects

Steven Johnson syndrome
Contraindication

Pregnancy and baby – Kernicterus
Unknown
Spectrum of Activities
1. Highly active blood schizontycide
2. Gametocidal to
a. P.vivax
b. P.ovalae
c. NOT P.falciparum
Tetracycline
 Contraindication in pregnancy and baby
due to permanent teeth discoloration

Binds to 30S ribosomal subunit

Blocks tRNA binding to A site
Spectrum of Activities

Slow acting blood schizonticides
Acts by interfering with the parasitic mitochondrial
function
Atavaquone
Primaquine
 Contraindicated in G6PD deficiency

Production of free radical in the food vacoules

Inhibition of Ca2+ ATPase pump of the parasite
Spectrum of Activities

Rapidly acting blood schizonticide

Sulfadoxine inhibits Dihyropteroate Synthase
enzyme

Pyrimethamine inhibits the Dihydrofolate
Reductase enzyme
Spectrum of Activities

Slow acting blood schizonticide
Unknown
Spectrum of Activities

The only antimalarial can fight againt hepatic
latent and primary stage

No activity against erythrocytic stage
Central Nervous System
Drug Classes
Drugs
Strong Opioid Agonist
Opioid Analgesic and
Antagonist
Partial Opioid Agonist
Morphine
Fentanyl
Methadone
 less severe withdrawal syndrome
 use in management of
dependency
Meperidine
 Used in Biliary colic
Codeine
Dextrometorphan
Pentazocine
Mixed Receptor Agonists
Opioid Antagonists
Naloxone
 Used in Opioid toxicity NOT
dependency
Tramadol
Other Non-Opioid Analgesic
Mechanism of Action


Strong µ (Mu) agonist
Variable affinity towards
o
o k (Kappa) receptor
Strong k (Kappa) receptor agonist
Antimuscarinic
o Distinctive anticholinergic effect
Partial agonist of µ (Mu) receptor
 Suppress cough center at Medulla Oblongata
 Partial µ (Mu) receptor
 Antagonist the activity of NMDA glutaminergic receptor
 Inhibit reuptake of serotonin
 k (Kappa) receptor agonist
 Antagonist in
o µ (Mu) receptor

Inhibits all opioid receptors
 µ (Mu) receptor

 k (Kappa) receptor
 Weak µ (Mu) receptor agonist
 Moderate Serotonin Reuptake Transporter (SERT) inhibitor
 Weak Norepinephrine Reuptake Transporter (NET) inihibitor


Central Nervous System
Drug Classes
Drugs
Mechanism of Action
Phenytoin

CYP450 Inducer

Contraindicated in pregnancy – Fetal Hydantoin
syndrome

Narrow Therapeutic Index

Follow zero order elimination

Displace drugs from Albumin
Side Effects

Nystagmus

Ataxia

Diplopia

Gingvial hyperplasia
Carbamazepine

CYP450 Inducer

Contraindicated in pregnancy
 Blocks the activated state of Na+ voltage channels
 ↓synaptic release of Glutamate
Indication
 Generalized tonic-clonic/ Gran mal seizure
 Partial seizures
Should not be given in Absence seizures
Valproic Acid

CYP450 Inhibitor

Displace Phenytoin from Albumin

Contraindicated in pregnancy

Felbamate

Block of NMDA receptors

↑GABAA receptor responses
Indications

Partial seizures

Generalized seizures
↓the low-threshold current of Ca2+ T-type channels
Indication

Absence seizure

↑phasic GABAA phasic receptor
Indications

Generalized tonic-clonic/ Gran mal seizure Partial seizures
responses

Generalized seizures

↓excitatory synaptic responses

Neonatal seizures


Status epilepticus
↑phasic GABAA phasic receptor responses
Clonazepam
Indication

Absence seizures
Diazepam

Myoclonic seizure

Status epilepticus

Infantile spasm

Blocks the activated state of Na+ voltage

Partial seizures
channels

Generalized seizures
Indications

Absence seizures

Generalized tonic-clonic/ Gran mal seizure

Prolong inactivation of Na+ voltage channels

Partial seizures

Blocks presynaptic Ca2+ voltage channels

Generalized seizures

↓release of Glutamate

Absence seizures
Indications

Myoclonic seizures

Generalized tonic-clonic/ Gran mal seizure
Antiepileptic Drugs
Ethosuximide
Phenobarbital
Bezodiazepine
 Diazepam
 Clonazepam
Topiramate
Lamotrigine


Blocks the activated state of Na+
voltage channels
Blocks the NMDA receptors
↑GABA level in the brain
Indication

Generalized tonic-clonic/ Gran mal seizure Partial seizures

Generalized seizures

Absence seizures

Myoclonic seizures
Central Nervous System
Drug Classes
Drugs
Barbiturate – Thiopental

Contraindicated in
o Severe hypotension
o Addison disease
o Liver disease
o Breathing disorder
General Anasthesia
Mechanism of Action




Lipid Solubility-Anaesthetic Potency Correlation (the Meyer-Overton
correlation)
Lipid Hypotheses of General Anaesthetic Action
Modern Lipid Hypotheses
Membrane Protein Hypothesis of General Anaesthetic action
Benzodiazepine

Contraindicated in
o Pregnancy
o Myasthenia gravis
o COPD
Propofol
Etomidate
Ketamine
 Contraindicated in ICP

Amide


Local Anasthesia

Ester
Anti-Parkinsonism

Medium action
o
Lidocaine
Long action
o
Bupivacaine
Short acting
o
Procaine
Long action
o
Tetracaine
Surface acting
o
Cocaine
Inactivation of Sodium channel trhough closure of M type channel and
eliciting Potassium influx
Levodopa

Given with carbidopa to inhibit the action of peripheral DOPA
Decarboxylase
MAOb Inhibitor

Selegiline
COMT Inhibitor

Tolcapone – not used anymore due to severe Hepatotoxicity

Entacapone
Dopamine Receptor Antagonist

Bromocriptine
Other Usage

Hyperprolactineamia

Galactorrhea

Amenorrhea

Type 2 Diabetes Mellitus
L-Dopa is the precursor of Dopamine; therefore by administering L-Dopa with
hope it will increase the level of Dopamine in the brain
Anticholinergic Agent

Benzatropine
Antagonises the effect of acetylcholine, decreasing the imbalance between the
neurotransmitters acetylcholine and dopamine
Covalently bind to MAOB and leads to irreversible inhibition of the activity of the
enzyme
COMT inhibitors are somehow similar to that of Carbidopa, in a sense that COMT
inhibitors inhibit the activity of COMT in the periphery as well as in the brain
Potent agonist at dopamine D2 receptors and various serotonin receptors
Central Nervous System
Drug Classes
Sedatives and
Hypnotics
Drugs
Hypnotics
Anxiolytics
Typical
Antipsychotic
Antipsychotic and
Lithium
Atypical
Antipsychotic
Mood Stabilizer
Antidepressant
Mechanism of Action
Barbiturate – Phenobarbital
 CYP450 Inducer
Side Effects
 Hangover syndrome
 Dependence
 Withdrawal syndrome
 Tolerance
Benzodiazepine – Clonazepam
 Flumazenil used in Benzodiazepine toxicity
Increase the mean open time of GABA-A activated chloride channels
Newer Hypnotics

Zolpidem
Buspirone
Selectively binds to the Alpha1 site on the GABA receptors
Haloperidol
Side Effects

Extrapyramidal side effects
o
Acute dystonia
o
Akathasia
o
Parkinsonism
o
Tardive dyskinesia

Nacoleptic Malignant Syndrome
Clozapine
Side Effects

Agranulocytosis

Cardiac toxicity

DKA
Lithium

Narrow Therapeutic Index
Side Effects

Diabetes Insipidus

Thyroid toxicity
Competitively inhibits the D2 receptors
Binds to Alpha1 and Alpha2 Benzodiazepine sites on the GABA receptors




Partial agonist of the 5-HTA1 Serotonin receptors
Has also affinity towards
o
D2 Dopaminergic receptors
Preferentially inhibit D4 receptor
Partial agonist of 5-HT1A and 5-HT1B
Attenuate the signalling via Phosphotidyl Biphosphate (PIP2) 2nd messenger coupled
receptors
Tricylic Antidepressant

Primary Amine – Amitriptylline

Secondary Amine – Desipramine

MAO Inhibitor – Phenelzine

Serotonin syndrome if given with SSRI

Cheeze effect when taken with tyramine containing foods
Selective Serotonin Reuptake Inhibitor – Fluoxetine
Serotonin/Norepinephrine Reuptake Inhibitor – Venlafaxine
Atypical Antidepressant – Bupropion
Nonselective MAO A and MAO B inhibitor
Inhibition of Norepinephrine and Serotonin reuptake
o
Inhibit presynaptic transporters

Serotonin Transporter (SERT)

Norepinephrine Transporter (NET)
SELECTIVELY inhibits the action of Serotonin Transporter (SERT)
Potent inhibitor of SERT and NET

Inhibits the reuptake of Norepinephrine and Dopamine

Stimulates the release of Dopamine and Norepinephrine from the
presynaptic terminal
Urinary
Drug Classes
Treatment of UTI
Drugs
Fluoroquinolone
(Bacteriocidal)
 Contraindicated
in
o Pregnancy
o Children
below 18
years old
Side Effects
 Photodermatitis
 Abnormal bone
and cartilage
growth
 Tendonitis
 CNS toxicity
 CVS toxicity
Nalidixic Acid
 Gram Negative except
Quinolone
P.aeruginosa
 No Gram Positive
Ciprofloxacin (2nd Generation)
 Gram Negative
 Gram Positive except Strep.
Pneumoneae
Levofloxacin (2rd Generation)
 Gram Negative
Flouroquinolone
 Gram Positive
 Atypical bacteria
Moxifloxacin (4th Generation)
 Gram Negative
 Gram Positive
 Atypical Bacteria
Nitrofurantoin (Bacteriocidal)
 Contraindicated in pregnancy and G6PD
Uroseptic
Fosphomycin (Bacteriocidal)
Aminoglycosides
Aminoglycosides,
Sulfonamides and
Trimethoprim
Streptomycin, Gentamicin
 Post antibiotic effect, use loading dose
Trimethoprim and Sulfamethoxazole (Bactrim)
 Contraindicated in
o pregnancy and infant – Kernicterus
o G6PD
 Ratio 1:5, trimethoprim and sulfonamide
Mechanism of Action
Inhibits DNA Gyrase and Topoisomerase IV
This electrophilic intermediate will non-specifically
attack
o Bacterial ribosomal protein
o DNA
o Respiration
o Pyruvate metabolism
o Other macromolecules
o Inhibition of protein synthesis
The first stage of cell wall synthesis takes place in the
bacterial cytoplasm
It binds to the 30S Ribosomal Subunit of bacteria, thus
inhibiting protein synthesis
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

Sulfonamide inhbits Dyhropteroate Synthase
Trimethroprim inhibits Dihydrofolate Reductase