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31 Cards in this Set
- Front
- Back
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Aminophylline
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a methyl xanthine
80% theophylline 20% ethylene diamine |
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Theophylline
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a methyl xanthine
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methyl xanthines help with...
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broncho-spasms
Nocturnal asthma |
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Theophylline inhibits...
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phosphodiesterase
remember: phosphodiesterase breaks down cyclic amp...so if I inhibit PDE, i increase cAMP...this will lead to things that will help bronchodilate |
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Theophylline antagonizes...
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the adenosine receptor on adenylate cyclase...therefore PDE can't do it's thing...(I think)
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Pharmacodynamics of methyl xanthines
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*relaxes smooth muscle (vasodilates/bronchodilates)
*CNS: increases stimulation *CVS: increases myocardial contractility, vasodilates, and reduces PVR *Skeletal muscle: reduces fatigue *Kidneys: diuresis Increased pepsin and gastric acid Metabolism: increases basal metabolic rate and FFA |
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Theophylline toxicity
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Early CNS: anxiety, tremor, insomnia
GI: nausea, vomiting CVS: tachycardia, palpitations, arrhythmias, hypotension CNS effects: twitching, seizures Metabolic |
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Theophylline therapeutic monitoring
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poor clinical indicators of efficacy/toxicity
narrow therapeutic range action proportional to concentration variable phamacokinetics reasonable half-life relatively rapid easy HPLC assay |
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Cromokalin derivatives
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anti-inflammatory drugs:
sodium cromoglycate Nedocromil |
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Glucocorticosteroids
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Anti-inflammatory drugs
2 types inhaled and systemic |
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Inhaled steroids
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anti-inflammatory:
Beclomethasone |
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Systemic steroids
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Anti-inflammatory:
hydrocortisone, prednisone, prednisolone, methylprednisolone |
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Sodium cromoglycate and Nedocromil
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anti-inflammatory drugs:
cromokalim |
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Uses of Sodium Cromoglycate
(Cromolyn) |
prophylaxis in antigen and exercise induced asthma
allergic rhinitis and conjunctivitis |
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Mechanism of sodium chromoglycate
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*not a direct bronchodilator
*inhibits the release of inflammatory mediators from mast cells in particular *suppresses effects of kinins on inflammatory cells *inhibits sensory C-fiber endings? (reduced cough?) |
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Side effects of Sodium cromoglycate
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VERY SAFE!!!
he says it's one of the safest drugs on the market cough and wheeze headache, nausea |
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Uses of corticosteroids:
SYSTEMIC THERAPY |
acute severe asthma (status asthmaticus)
chronic maintenance therapy |
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Use of corticosteroids:
INHALED THERAPY |
prophylaxis in mild/moderate asthma
can be combined with systemic steroids in chronic severe asthma to reduce systemic steroid requirements use when people have worsening of their noctural syndromes |
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Which enzymes do glucocorticosteroids inhibit?
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enzymes producing PGs, LTs, and TX, eg. PLA2 via lipocortin, COX-2
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Glucocorticosteroids inhibit the transcription of...
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pro-inflammatory cytokines eg. IL-1, TNF-alpha, G-MCSF, IL-3, and IL-4, 5, and 6
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Glucocorticosteroids directly counteract...
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the positive effects of several cytokines on transcription factors AP-1 and NF-KB
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Glucocorticoids induce the enzymes...
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ACE and NEP which degrade bradykinin and tachykinin
(bradykinin is a bronchoconstrictor) |
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Glucocorticosteroids increase...
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beta 2 and NK1 receptor transcription
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Glucocorticosteroids reduce cell trafficking by...
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inhibiting effects of TNF etc and reduces the expression of cell adhesion molecules...
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Glucocorticoids induce apoptosis in...
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eosinophils
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Vasocortin!!!!
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the antipermeability factor that glucocorticoids stimulate the synthesis of...this inhibits plasma exudation from venules
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Pharmacokinetics of the inhaled steroids
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inhaled route:
about 10% of dose reaches bronchi 90% of dose is swallowed metabolism: hepatic CYP3A low systemic circulations |
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Side effects/toxicity of inhaled glucocorticoids
(just local effects) |
Thrush - C. Albicans (10-15% of patients)
Dysphonia - hoarse voice (causes a local myopathy) |
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Side effects/toxicity of inhaled glucocorticoids
(systemic effect: at doses of about 1600 mcg/day Beclomethasone) |
HPA axis suppression
Bruising/Purpura Cataracts Inhibits bone growth (?children?) Hypercholesterolemia Hyperglycemia Behavioral disturbances |
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Side effects of systemic glucocorticoids
(Acute) |
CNS- insomnia/psychosis
Metabolic- 1) hyperglycemia and 2) Na and H20 retention Proximal myopathy Suppress signs of infection |
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Side effects of systemic glucocorticoids
(chronic) |
HPA axis suppression
(adrenal suppression) Cushing's appearance Peptic ulcer Opportunistic infection Osteoporosis Growth suppression (kids) Pancreatitis Aspetic necrosis of the femoral head |
