Autacoids Drugs Flashcards
What is the generic name of Diphenhydramine?
Benadryl and sominex
Which of the antihistamines is first generation?
diphenhydramine
which of the antihistamines has significant antimuscarinic activity?
diphenhydramine
What is the mechanism of action of diphenhydramine?
H1 receptor antagonist–> reduces histamine response via H1 receptors in GI tract, blood vessels, bronchial muscle, uterus and suppresses the formation of edema, flare and pruritius
What are some of the adverse reactions to diphenhydramine?
CNS: confusion, dizziness, and sedation
Antimuscarinic: mydraiss, xerostomia, reduced bronchial secretions, tachycardia, constipation, urinary retention
What are the precautions of diphenhydramine?
asthma heart disease hepatic disease (CYP2D6) glaucoma bladder obstruction, urinary retention Infants
What are the 2nd generation antihistamines?
Cetrizine, fexofendine, and loratadine
What is the generic name of Cetrizine?
zyrtec
What is the mechanism of action of cetrizine?
H1 receptor inverse agonist–> reduces histamine response via H1 receptors in GI tract, blood vessels, bronchial muscle, uterus and suppresses the formation of edema, flare and pruritius
What are the adverse reactions of cetrizine?
few adverse reactions:
CNS: sedation, fatigue
Xerostomia
What are the precautions of cetrizine?
If creatinine clearance is
What is the brand name of Fexofenadine?
allegra
What is the mechanism of action for fexofenadine?
H1 receptor inverse agonist–>
reduces histamine response via H1 receptors in GI tract, blood vessels, bronchial muscle, uterus and suppresses the formation of edema, flare and pruritus
What are the adverse reactions to fexofenadine?
few adverse reactions:
GI: nausa, dyspepsia
CNS: drowsiness and sedation
What are the precautions for fexofenadine?
decrease dose in patient with decreased renal function
avoid taking with fruit juices
What are the brand names of loratadine?
Claritin and Tavist
What is the mechanism of action for loratadine?
H1 receptor inverse agonist–>
reduces histamine response via H1 receptors in GI tract, blood vessels, bronchial muscle, uterus and suppresses the formation of edema, flare and pruritus
What are the adverse reactions to loratadine?
few
CNS: headache and sedation
Xerostomia
What are the precautions of loratadine?
Hepatic disease
if creatinine clearance is
What is a H2 antagonist example?
Cimetidine
What is Cimetidine indicated for?
GERD, peptic ulcer disease and intermittent dyspepsia
What is the mechanism of action from Cimetidine?
Inverse agonist–> reduces the constitutive activation of H2 receptors on parietal cells
What are the adverse reactions to Cimetidine?
headaches
rare blood dyscrasias
What are the precautions for Cimetidine?
hepatic disease
renal insufficiency
What are two drugs that are used to treat migraines?
Ergotamine
Sumatriptan
What is the MOA of Ergotamine?
Binds to many Serotonin receptors to have partial agonist or antagonist activity--. vasoconstriction of arteries and veins and decreased blood flow to extremities AND Oxytocic agent (activates oxytocin)
What are the adverse reactions to Ergotamine?
GI: NVD, xerostomia
Ergotism: angina, asthenia, coronary vasospasm, cramps, myalgia, paresthesias, changes in HR and vasoconstriction that may result in hypothermia or tissue necrosis
What are precautions of Ergotamine?
CV VASCULAR DISEASE: MI, STROKE HEPATIC DISEASE RENAL FAILURE PREGNANCY
Which migraine medication is FDA category X?
Ergotamine
What is Sumatriptan indicated for?
Acute migraines
What is the MOA of Sumatriptan?
Agonist at presynaptic 5-HT1D autoreceptors and at vascular 5-HT1B receptors –> vasoconstriction
What are the Adverse reactions to sumatriptan?
potentially fatal CV events
GI: NVD, vasospastic effects
Injection site burning and pain
What are the precautions for sumatriptan?
CV
ISCHEMIC BOWEL DISEASE
hepatic disease
renal insufficiency
what are the main uses of hydrocortisone?
anaphylaxis, asthma, COPD, inflammatory bowel disease, rheumatic disorders, and dermatoses
What is the MOA of hydrocortisone?
represses COX-2 expression–> decreases cytokine production, decreased formation and release of inflammatory mediators, causes apoptosis for eosinophils
What are the adverse reactions to hydrocortisone?
essentially none, but prolonged used may cause cataracts and exacerbate glaucoma and prolonged use will need to be tapered off
What are the precautions of hydrocortisone?
ABRUPT DX OF PROLONGED SYSTEMIC THERAPY
CUSHINGS SYNDROME
pre-existing bacterial, viral and fungal infections
What are some of the indications for Prednisone?
autoimmune disorders, allograft rejection, asthma, IBD, rheumatoid arthritis, etc
What is prednisone a pro-drug for?
Prednisolone
What is the MOA of prednisone?
represses COX-2 expression–> decreases cytokine production, decreased formation and release of inflammatory mediators, causes apoptosis for eosinophils
What are the adverse reactions to prednisone?
CNS: headaches, insomnia, vertigo, depression, anxeity, euphoria, personality changes and psychosis
GI: NVD, anorexia and gastritis
Cataracts
Opportunistic infections
What are the precautions for prednisone?
CUSHING’S SYNDROME
HIGH DOSES AND LONG-TERM THERAPY CAN SUPPRES HYPOTHALAMIC-PITUITARY-ADRENAL SYSTEM
preexisting bacterial, viral and fungal infections