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Chapter 6 TDM 2
Chapter 6 TDM 2
pulmonary disease
First phase :
bronchoconstriction
bronchodilators
Second phase : inflammation
steroids
For moderate or severe asthma
attacks
Bronchodilator, vasodilator
Stimulates respiration and
strengthens the action of
cardiac muscles
CNS stimulant
Oral or IV form
Pharmacokinetics
Metabolite: 3-methyl-xanthine
Drug interactions:
Phenytoin, carbamazepine
Erythromycin
Adult therapeutic range: 10-20ug/mL
Newborns : 5-10ug/mL
Toxicity :
15-20 ug/mL
Nausea, vomiting, headache and
anxiety
20-40 ug/mL
Tachycardia, arrhythmias
>40 ug/mL
Seizures, cardiac arrest
Tissue damage ---arachidonic acid
1. lipo-oxygenase pathway
> leukotrienes
2. cyclo-oxygenase pathway
> thromboxanes
> prostaglandins
*** Inflammation
Block the cyclo-oxygenase
pathway
Anti-inflammatory
Fluid retention, weight gain,
osteoporosis, gastrointestinal
bleeding and mental changes
Anti-inflammatory w/o
undesirable side effects
Acetaminophen/Paracetamol
Acetylsalicylic acid/Aspirin
Naproxen, Ibuprofen,
Piroxicam
Analgesic,antipyretic and anti-
inflammatory
Lower doses: anti-thrombotic
Chronic toxicity: tinnitus, muffled
hearing
Acute toxicity : acidosis
Reye’s syndrome: hepatotoxicity
Analgesic and anti-pyretic
Metabolites : glucoronide and
sulfate conjugates
Acute toxicity : nausea,
vomiting and abdominal pain
Chronic toxicity : anemia, renal
damage, GI disturbances
Autoimmune diseases
Tissue transplant recipient
1. Ciclosporin
2. Tacrolimus
3. Rapamycin
4. Mycophenolate mofetil
5. Leflunamide
Ciclosporin
Drug of choice for maintenance
of kidney, liver, heart and heart-
lung allografts
Adverse effect : nephrotoxicity
Other effects : neurologic,
dermatologic, hepatotoxic
Tacrolimus
Currently used in transplant
surgery to prevent organ rejection
Similar toxicity profile to
ciclosporin
Available as citrate and CO3 salts
Anti-manic agents
Prophylaxis and treatment of
bipolar disorder
Toxicity : from single toxic dose or
prolonged use
Renal toxicity and hypothyroidism
Block reuptake of adrenergic and
dopaminergic neurotransmitters
Amitriptyline, imipramine,
nortriptyline, despramine, doxepin
Toxicity: excess CNS stimulation -
seizures, coma, hypotension,
respiratory depression
Inhibits dihydrofolate reductase
(DNA synthesis)
Uses :
Psoriasis
Refractory rheumatoid arthritis
Malignant neoplastic diseases
Toxicity : hematologic effects, GI
effects
Treat leukemias and lymphomas
prior to BM transplantation
Toxicity : hepatic veno-occlusive
disease