Term
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Definition
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Term
Histamine Receptors:
G protein coupled receptors
H1: Primarily coupled to ___ and activate intracellular ___ release via __ pathway
H2: Primarily coupled to __ and activate ___ & increase ___ |
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Definition
Gq
Ca2+
IP3
Gs
adenylyl cyclase
cAMP |
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Term
| H__ receptor is involved in acid release in GI tract. |
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Definition
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Term
| H__ and H__ are G protein coupled receptors |
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Definition
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Term
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Definition
smooth muscle
glands
endothelial cells
brain
heart
skin |
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Term
Physiological Effects: H1
_____ (asthmatics)
_____ excretion -> nasal and bronchial mucus
Increased _____ permeability
Intestinal ____ contraction
Stimulation of ____ nerve endings
____: release of NO: initial response |
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Definition
Bronchoconstriction
Exocrine
capillary
smooth muscle
sensory
Vasodilation |
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Term
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Definition
Gastric parietal cells
Vascular smooth muscle
heart
mast cells
brain |
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Term
Physiological Effects: H2
____ secretion
Positive ___ & ____ response
Slow, sustained ____ |
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Definition
Gastric acid
chronotropic & inotropic
vasodilation |
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Term
Allergic histamine Release:
____ hypersensitivity reaction
Ig___ antibodies bound to ___ & _____
Allergen re-exposure triggers release
Other inflammatory mediators are released, PAF, LTD4, PGD2, etc. |
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Definition
Immediate
E
mast cells and basophils |
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Term
Non-allergic histamine release:
Clinical concern- anaphylactoid reactions
-> ____- tubocurarine, morphine, succinylcholine, radiocontrast media, plasma expanders, vancomycin
-> ____ & _____
-> ____ - cold, trauma, sun-exposure |
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Definition
Drugs
Venoms and toxins
Cell injury |
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Term
Histamine: Clinical Uses
______ only
Assessment of ____ reactivity, asthma -> ____ - more commonly used
Patient breathes in challenge: nebulized drug. Spirometry performed. |
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Definition
Diagnostic
bronchial
Methacholine |
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Term
| H1 Antagonists- Indications: (3) |
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Definition
Adjunct in treatment of anaphylactic shock
Urticaria and pruritis
Rhinitis |
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Term
| H2 Antagonists-Indications (3) |
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Definition
Reduction of acid secretion in stomach
Peptic ulcer
GERD |
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Term
H1 Receptor Antagonists Pharmacokinetics:
____ absorbed
____ Vd
*___ generation drugs do not cross BBB to any extent
metabolized in the liver
t1/2 most drugs = __-__ hours
sustained release preparations t1/2= __-__ hrs |
|
Definition
rapidly
large
2nd
4-6
12-24 |
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Term
1st Generation H1 Antagonists are “dirty” drugs, also block:
____ receptors –> sedation, drying, dysuria
____ receptors
____ receptors -especially cyproheptadine -> sedation
some drugs block ___ channels -> local anesthetic effects |
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Definition
muscarinic
a-adrenergic
5-HT
Na+ |
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Term
| What 1st generation H1 antagonists particularly block the 5-ht receptor? |
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Definition
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Term
| What 1st generation H1 antagonists particularly block the a-adrenergic receptor? |
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Definition
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Term
| What 1st generation H1 antagonists particularly block the muscarinic receptor? |
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Definition
diphenhydramine
clemastine
promethazine |
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Term
| First Generation H1 Antagonists: Clinical Indications (4) |
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Definition
Acute and Chronic Allergic Rhinitis
Vasomotor rhinitis
Eosinophilic nonallergic rhinitis
Viral Upper Respiratory Infection |
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Term
| Rhinitis Symptoms Treated By 1st Generation H1 Blockers (3) |
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Definition
Sneezing (H1)
Itching (H1)
Rhinorrhea (m) |
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Term
| _____ is NOT treated By 1st Generation H1 Blockers |
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Definition
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Term
| ____ Generation H1 Blockers are better at treating runny nose. |
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Definition
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Term
| First Generation H1 Antagonists: Clinical Indications contd. (5) |
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Definition
Urticaria
Allergic conjunctivitis
Anaphylactic reactions -> adjunct to epinephrine
Motion sickness and nausea (H1 and m)
Insomnia (H1 and m) |
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Term
Motion sickness: _____ (muscarinic antagonists), drugs that antagonize ___ receptors are also effective
Vomiting center has lots of receptors: ___ & ___ receptors |
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Definition
scopalamine
H1
H1 and muscarinic |
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Term
| Dimenhydrinate is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Diphenhydramine is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Cyclizine is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Hydroxyzine is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Meclizine is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Chlorpheneramine is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Promethazine is what type of drug? |
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Definition
| 1st generation H1 antagonists |
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Term
| Side Effects- First Generation H1 antagonists: (5) |
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Definition
Sedation - antimuscarinic effect, antihistamine, (antiserotonin)
CNS
-> Dizziness, tinnitus, nervousness, fatigue
-> Paradoxical: insomnia
Dry mouth – (antimuscarinic effect)
Ocular- blurred vision (antimuscarinic effect)
Urinary retention - – (antimuscarinic effect) |
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Term
| Cetirizine is what type of drug? |
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Definition
| 2nd generation H1 antagonist |
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Term
| Levocetirizine is what type of drug? |
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Definition
| 2nd generation H1 antagonist |
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Term
| Fexofenadine is what type of drug? |
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Definition
| 2nd generation H1 antagonist |
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Term
| Loratidine is what type of drug? |
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Definition
| 2nd generation H1 antagonist |
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Term
| Desloratidine is what type of drug? |
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Definition
| 2nd generation H1 antagonist |
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Term
| 2nd generation H1 antagonists have ____ distribution to CNS (don’t cross BBB appreciably) –therefore, much less ____ compared to 1st generation drugs |
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Definition
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Term
| 2nd generation H1 antagonists Have ____ elimination t1/2 than 1st generation –therefore, ____ duration of action |
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Definition
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Term
| Rhinitis Symptoms Treated by 2nd Generation H1 antagonists: (2) |
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Definition
Sneezing (H1)
Itching (H1) |
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Term
| ____ & ____ is NOT treated by 2nd Generation H1 antagonists |
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Definition
Sinus Congestion
Rhinorrhea |
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Term
| Decongestants are ________ |
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Definition
| a-adrenergic agonists (Oral) |
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Term
| Decongestants cause ______ and reduce ____ |
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Definition
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Term
| Pseudoephedrine is what type of drug? |
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Definition
| a-adrenergic agonists (decongestant) |
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|
Term
| Phenylephrine is what type of drug? |
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Definition
| a-adrenergic agonists (decongestant) |
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Term
Oral Decongestants:
Reduce ____________
Reduce fluid in ________
DO NOT reduce _____,______, & _______
Commonly combined with an _______
Increases __________ -> Use with care (if at all) in patients with hypertension and other cardiovasular problems
Stimulating, may cause ______
_______ |
|
Definition
sinus congestion
Eustachian tubes
sneezing, itching, and rhinorrhea
antihistamine
blood pressure
insomnia
Mydriatic |
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Term
Other Therapy for Rhinitis:
Intranasal ______, ________
Inhibit degranulation of ___ cells |
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Definition
cromolyn sodium, nedocromil
mast |
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Term
| ____ + ____ can cause fatal arrhytmias b/c interactoins with ____. |
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Definition
Antihistamines + decongestants
CYP3a4 |
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Term
| principal clinical effect of H2 Receptor Antagonists is blockade of ________________ |
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Definition
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Term
| H2 Receptor Antagonists are very ___ - do not block ___ receptors |
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Definition
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Term
| H2 Receptor Antagonists may be used in severe _____, _____ |
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Definition
| anaphylactic reactions, shock |
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Term
| ___ receptors on ___ cells bind histamine and cause release of gastric acid into lumen. So if block __ recptors block acid release. |
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Definition
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Term
| Cimetidine is what type of drug? |
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Definition
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Term
| Ranitidine is what type of drug? |
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Definition
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Term
| Famotidine is what type of drug? |
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Definition
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Term
| Nizatidine is what type of drug? |
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Definition
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Term
| _____ :H2 agonist used to stimulate acid secretion in the stomach- measures gastric function |
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Definition
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Term
| Expectorants Facilitate ____ or decrease ____ of mucus to facilitate ____ of mucus secretions in airways. |
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Definition
secretion
viscosity
clearance |
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Term
| _____: claimed to facilitate removal of viscous mucus. |
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Definition
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Term
| Guaifenesin is what type of drug? |
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Definition
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Term
| _____: claimed to decrease viscosity of mucus. |
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Definition
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Term
| Potassium iodide is what type of drug? |
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Definition
|
|
Term
| _____- useful in cystic fibrosis. |
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Definition
| Recombinant DNAse (Dornase alpha) |
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Term
| Recombinant DNAse (Dornase alpha) is what type of drug? |
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Definition
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Term
| 2 classes of Antitussives: |
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Definition
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Term
| _____ : work via central suppression of cough reflex |
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Definition
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Term
| Codeine is what type of drug? |
|
Definition
| opioid (used as anntitussive) |
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Term
| Dextromethorphan is what type of drug? |
|
Definition
| opioid (used as anntitussive) |
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Term
| Dextromethorphan is an ___ drug, lacks ____ properties |
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Definition
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Term
| Benzonatate is what type of drug? |
|
Definition
| non-opioid (used as an antitussive) |
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Term
| Benzonatate is a ______ (____); central? |
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Definition
|
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Term
| what antihistamine (non-opioid) is also used as an antitussive? |
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Definition
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