Antihistamine & Nasal Steroid

Front 1

1. What are 2 things that degrade histamine?
2. What converts histidine to histamine?
3. Which can cross BBB

Back 1

1. Histamine Methyltransferase & Diamine oxidase -> not recycled
2. Histidine decarboxylase - not rate limiting
3. Histidine, histamine can't

Front 2

Histamine comes from venoms, red wine, swiss cheese, fish bacteria Sx like an allergic rxn

Endogenous - 98% from Basophils and mast cells also histaminergic neurons

Back 2

4 Histamine receptors, all are G protein-coupled

Front 3

1. What histamine R are clinically imp and why?
2. Blocking CNS histamine 1 receptors causes what?

Back 3

1. H1 is allergic rxn (wheezing, sneezing, itching), causes bronchoconstriction, gastric constriction...
H2 - ^ gastric acid secretion
2. Sedation and reduced attention

Front 4

1. What does histamine doe to smooth m?
2. Circulatory effects?
3. GI effects
4. CNS effects

Back 4

1. Increases smooth m. contraction, esp in the bronchi and gut
2. Vasodilatio (red skin), release of NO (drop BP), increase vascular permeability - tissue swelling
3. ^ Gastric acid and pepsin secretion and ^ motility
4. n. ending itchy; arousal, attention, NT regulator, higher in the day

Front 5

1. Allergens, injury, drugs trigger granule release of?
causes swelling, edema, iching, pain, erythema, difficulty breathing, drop BP, CV effects
2. Indication of antihistamine?

Back 5

1. Histamine esp by mast cells
2. Relief of allergic Sx (sneezing, runny nose, red itch tearing eyes, itch skin) caused allergic rhinitis, urticaria other skin allergies

Front 6

1. How are antihistamines given?
2. Time to peak concentration? Duration?
3. Primary route of elimination?

Back 6

1. well absorbed orally
2. effective at 30 min, peak at 3 hrs, last up to 24 hrs
3. Hepatic

Front 7

1. Ending of 2nd gen antihistamines?
2. Characteristics of first gen drugs?
3. added indication of 1st gen?

Back 7

1. -adine or izine
2. Cross BBB (CNS effects), Cross react w/ other receptors esp muscarinic cholinergic receptors
3. motion sickness/nausea & sleep aid

Front 8

Effect on 1st gen antihistamine on:
1. H1R
2. Muscarinic R
3. Alpha-adrenergic R
4. 5 serotonin R
4. IKr channel

Back 8

1. Decreased allergies peripherally, CNS ^ sedation,
2. ^ dry mouth, urinary retention, sinus tachycardia
3. Hypotension, dizzy, reflex tachycardia
4. ^ appetite, antiemetic effects
5. Prolonged QT interval, mb Vent. arrhythmia

Front 9

1. Pt presents w/ hot dry and flushed skin, dry mucous membrane, ^ temp, dilated pupils, blurred vision, disorientated, what to think?
2. what is an OTC ethanolamine used to relive allergy Sx, sleep aid, less for motion sickness?

Back 9

1. 1st gen overdose
2. Diphenhydramine - SE: powerful anticholinergic effects, drowzy, sedated, often used in combo 1/2 life 6-8 hrs

Front 10

1. An OTC alkylamine, CNS stimulation due to SNRI activity so less drowsy then diphenhydramine, often used w/ opiods for cough suppression
2. a 1st gen phenothiazine, causes seziure in higher dose, respiratory depression in children < 2, used for allergies, nausea and motion sickness

Back 10

1. Chlorpheniramine maleate - 24 hr 1/2 life
2. Promethazine

1st gen Antihistamines decrease psychomotor performance, & increase sedation

Front 11

1. Major improvement of 2nd gen antihistamines?
- less toxic, b/c more specific
SE: fatigue,depression, peripheral anti-cholinergic effects at higher doses, cardiac arrhythmia

Back 11

1. Do not cross the BBB so no sedative or other CNS effects
--also low or no anti-cholinergic or alpha adrenergic so no or little dry mouth, urination dysfxn, tachycardia wt ^

Front 12

1. Example of a Piperidine, selective peripheral H1receptor antagonist; rapidly absorbed PO, 60% protein bound, minimal degradation 1/2 = 14 hrs,
2. What is 1 an active ingredient of?
--2nd gen antihistamine

Back 12

1. Foxofenadine
2. Terfenadine - a drug that was removed from market due to drug interxn

Front 13

1. Example of a pieperadine; competitive antagonist of H1 receptors, low SE. absorbed well PO, bound to plasma protein, Max concentration in 1 hr, **1st pass eliminated**
2nd gen

Back 13

1. Loratadine (8hrs) and desloratadine (27 hrs)

Pseudoephedrine provides more relief of Sx

Front 14

1. 2nd gen piperazine, metabolite of hydroxyzine, some penetration of BBB, no anti-cholinergic activity
SE: dry mouth, drowsy, nightmare, Headache
Nasal steroids - available as aerosol or spray, have steroids, work by reducing swelling & inflammation

Back 14

1. Cetirizine -> lasts up to 21 hrs avg 1/2 life 8 hrs; excreted through the kidneys
Nasal steroids -> indicated for allergic nasal Sx

Front 15

1. MA of Pseudoephedrine - also used for wt loss or a stimulant, Rx of drug induced hypotension
2. MA of phenylephrine? - Rx hypotension, mydriatic to dilate pupils
3. MA of Oxymetazoline - Rx nose bleed, decrease mucus, overuse leads to rebound congestion

Back 15

1. Indirect adrenergic agonist, ^ release of endog. NE; increases vasoconstriction @ a1-AR; few CNS effects
2. Direct a1-AR selective agonist; causes vasoconstriction -> decongestant, less effective than pseudoephedrine,
3. 12 hr relief; activates a1 and partially a2 ARs

Front 16

Pseudoephedrine - SE:
CNS stimulation - insomnia, nervous, excite, dizzy, anxiety
CV - ^ HR, arrhythmia, HTN, stroke risk
CI: DM, hyperthyroidism, CV disease, HTN, CAD
anxiety MAOI, pregnancy

Back 16

Phenylephrine
Pharmaco - metabolized by MAO in liver, 1/2 = 2-4 hrs
SE: HTN Insomnia nervousness
CI: HTN, use of MAOi, hrt disease

Front 17

1. What is COdeine used for?
2. Active metabolite blocks NMDA receptors, acts on mu opioid receptors
3. An expectorant drug; often combined w/ 2 and/or acetaminophen and/or ephedrine or phenylephrine

Back 17

1. Antitussive (cough) - mu receptor
2. Dextromethorphan
3. Guaifenesin

Front 18

1. Drugs FDA recommends to not give < 6yo? b/c there have been some deaths

Back 18

1. Decongestants, anthistamines, and antitussives