NR566 Final Exam Study Guide
Week 5
Chapter 56
H1 antagonists diphenhydramine, promethazine
o Adverse Effects
Sedation
Nonsedative CNS effects: Dizziness, incoordination, confusional
states, fatigue
GI effects: N/V/D or constipation, loss of appetite
Anticholinergic effects: Drying of mucous membranes, urinary
hesitancy, constipation, and palpitations
o Indication: Drug Selection
All of the H1 antagonists are useful in treating allergic disorders
Some are also indicated for other conditions (motion sickness,
insomnia)
Mild allergy
Motion sickness: Promethazine, dimenhydrinate
Insomnia: Diphenhydramine, pyrilamine
o Sleep aids
Practically all OTC sleep aids contain an H1 antagonist
(diphenhydramine or pyrilamine) as its active ingredient
o Lifespan Considerations
Infants: Can cause sedation
May be used in children older than 6 months with caution
Children/adolescents: Can be used safely in smaller doses
Pregnancy: Many antihistamines should be avoided unless
necessary
Breastfeeding: Occasional, small doses of antihistamines do not
appear to cause sedations in infants. Use caution
Older adults: Many should be avoided in older adults
Can make glaucoma or BPH worse
o 1st Generation Vs. 2nd Generation
2nd-gens produce much less sedation than first-gens because:
2nd-gen agents cross the blood-brain barrier poorly
They have a low affinity for H1 receptors of the CNS
Fexofenadine- Food Drug Interactions (Antihistamine)
o Certain fruit juices (apple, orange, grapefruit) can reduce fexofenadine
absorption, possibly reducing therapeutic effects
o Do not drink fruit juices within 4 hours before dosing or 1-2 hours after
dosing
,Chapter 58
Glucocorticoids
o MOA
These drugs differ from most drugs in two ways:
Glucocorticoid receptors are located INSIDE the cell rather
than on the cell surface
Glucocorticoids modulate the production of regulatory
proteins rather than the activity of signaling pathways
Glucocorticoids penetrate the cell membrane bind with receptors
in the cytoplasm converting the receptor from an inactive form to
an active form Receptor-steroid complex migrates to the cell
nucleus binding to chromatin in DNA altering activity of target
genes
o Pharmacologic Effects
Effects on metabolism and electrolytes
High doses: Glucose levels rise
Anti-inflammatory and immunosuppressant effects
o Adverse Effects
Osteoporosis with resultant fractures
Infection (by suppressing host defenses)
Impaired wound healing
Hyperglycemia
Myopathy
Fluid and electrolyte disturbance
Growth delay
Psych disturbances
Cataracts and glaucoma
PUD
Iatrogenic cushing syndrome
Adrenal suppression
o Allergic Reaction Management
Glucocorticoid responses are delayed, so these drugs have little
value as SOLE therapy for severe allergic reactions (anaphylaxis)
Good for: Allergic rhinitis, bee stings, drug-induced allergies
Chapter 63
Intranasal Glucocorticoids
o Indications
Most effective drugs for prevention and treatment of seasonal and
perennial rhinitis
, These drugs can prevent or suppress the major symptoms of
allergic rhinitis: congestion, rhinorrhea, sneezing, nasal itching, and
erythema
o Allergic Rhinitis Management
Drugs available:
Glucocorticoids (intranasal)
Antihistamines (oral and intranasal)
Sympathomimetics (oral and intranasal)
o Adverse Effects
Drying of the nasal mucosa & a burning or itching sensation
Also may occur: Sore throat, epistaxis, headache
Antihistamines- 1st Generation Vs. 2nd Generation
o First-gen are sedating, 2nd-gen are nonsedating
Intranasal cromolyn sodium indications
o Treatment of allergic rhinitis
o The drug is best suited for prophylaxis and hence should be given before
symptoms start
Sympathomimetics
o MOA
Reduce nasal congestion by activating a1-adrenergic receptors on
nasal blood vessels
o Indications
Reduce nasal congestion by activating a1-adrenergic receptors on
nasal blood vessels
For allergic rhinitis: Only relieve congestion (not rhinorrhea,
sneezing, itching)
Also indicated to reduce congestion associated with sinusitis and
colds
o Adverse Effects
Rebound congestion
CNS stimulation (most common of the oral route): restlessness,
irritability, anxiety, insomnia
CV effects
Abuse
Dextromethorphan indications: Most effective OTC nonopioid cough medicine,
and also shown to help relieve pain
Montelukast
o MOA: Block binding of leukotrienes to their receptors
This allows the drug to relieve nasal congestion, although it has
little effect on sneezing or itching
o Indications: Originally approved for asthma, is now approved for
seasonal and perennial allergic rhinitis as well
Ipratropium bromide MOA
o Blockade of cholinergic receptors inhibits secretions from the serous and
seromucous glands lining the nasal mucosa and decreases rhinorrhea
Week 5
Chapter 56
H1 antagonists diphenhydramine, promethazine
o Adverse Effects
Sedation
Nonsedative CNS effects: Dizziness, incoordination, confusional
states, fatigue
GI effects: N/V/D or constipation, loss of appetite
Anticholinergic effects: Drying of mucous membranes, urinary
hesitancy, constipation, and palpitations
o Indication: Drug Selection
All of the H1 antagonists are useful in treating allergic disorders
Some are also indicated for other conditions (motion sickness,
insomnia)
Mild allergy
Motion sickness: Promethazine, dimenhydrinate
Insomnia: Diphenhydramine, pyrilamine
o Sleep aids
Practically all OTC sleep aids contain an H1 antagonist
(diphenhydramine or pyrilamine) as its active ingredient
o Lifespan Considerations
Infants: Can cause sedation
May be used in children older than 6 months with caution
Children/adolescents: Can be used safely in smaller doses
Pregnancy: Many antihistamines should be avoided unless
necessary
Breastfeeding: Occasional, small doses of antihistamines do not
appear to cause sedations in infants. Use caution
Older adults: Many should be avoided in older adults
Can make glaucoma or BPH worse
o 1st Generation Vs. 2nd Generation
2nd-gens produce much less sedation than first-gens because:
2nd-gen agents cross the blood-brain barrier poorly
They have a low affinity for H1 receptors of the CNS
Fexofenadine- Food Drug Interactions (Antihistamine)
o Certain fruit juices (apple, orange, grapefruit) can reduce fexofenadine
absorption, possibly reducing therapeutic effects
o Do not drink fruit juices within 4 hours before dosing or 1-2 hours after
dosing
,Chapter 58
Glucocorticoids
o MOA
These drugs differ from most drugs in two ways:
Glucocorticoid receptors are located INSIDE the cell rather
than on the cell surface
Glucocorticoids modulate the production of regulatory
proteins rather than the activity of signaling pathways
Glucocorticoids penetrate the cell membrane bind with receptors
in the cytoplasm converting the receptor from an inactive form to
an active form Receptor-steroid complex migrates to the cell
nucleus binding to chromatin in DNA altering activity of target
genes
o Pharmacologic Effects
Effects on metabolism and electrolytes
High doses: Glucose levels rise
Anti-inflammatory and immunosuppressant effects
o Adverse Effects
Osteoporosis with resultant fractures
Infection (by suppressing host defenses)
Impaired wound healing
Hyperglycemia
Myopathy
Fluid and electrolyte disturbance
Growth delay
Psych disturbances
Cataracts and glaucoma
PUD
Iatrogenic cushing syndrome
Adrenal suppression
o Allergic Reaction Management
Glucocorticoid responses are delayed, so these drugs have little
value as SOLE therapy for severe allergic reactions (anaphylaxis)
Good for: Allergic rhinitis, bee stings, drug-induced allergies
Chapter 63
Intranasal Glucocorticoids
o Indications
Most effective drugs for prevention and treatment of seasonal and
perennial rhinitis
, These drugs can prevent or suppress the major symptoms of
allergic rhinitis: congestion, rhinorrhea, sneezing, nasal itching, and
erythema
o Allergic Rhinitis Management
Drugs available:
Glucocorticoids (intranasal)
Antihistamines (oral and intranasal)
Sympathomimetics (oral and intranasal)
o Adverse Effects
Drying of the nasal mucosa & a burning or itching sensation
Also may occur: Sore throat, epistaxis, headache
Antihistamines- 1st Generation Vs. 2nd Generation
o First-gen are sedating, 2nd-gen are nonsedating
Intranasal cromolyn sodium indications
o Treatment of allergic rhinitis
o The drug is best suited for prophylaxis and hence should be given before
symptoms start
Sympathomimetics
o MOA
Reduce nasal congestion by activating a1-adrenergic receptors on
nasal blood vessels
o Indications
Reduce nasal congestion by activating a1-adrenergic receptors on
nasal blood vessels
For allergic rhinitis: Only relieve congestion (not rhinorrhea,
sneezing, itching)
Also indicated to reduce congestion associated with sinusitis and
colds
o Adverse Effects
Rebound congestion
CNS stimulation (most common of the oral route): restlessness,
irritability, anxiety, insomnia
CV effects
Abuse
Dextromethorphan indications: Most effective OTC nonopioid cough medicine,
and also shown to help relieve pain
Montelukast
o MOA: Block binding of leukotrienes to their receptors
This allows the drug to relieve nasal congestion, although it has
little effect on sneezing or itching
o Indications: Originally approved for asthma, is now approved for
seasonal and perennial allergic rhinitis as well
Ipratropium bromide MOA
o Blockade of cholinergic receptors inhibits secretions from the serous and
seromucous glands lining the nasal mucosa and decreases rhinorrhea