Lecture 3 Flashcards by Michellea Russell

What is the direction of the signal for the cough reflex?

Irritant sends a signal up the afferent nerve to the cough center in the brain then the efferent signal makes the epiglottis close.

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What are the targets for drugs to work on the cough reflex?

Sensory receptors
Cough center
There is no evidence that drugs work on the afferent and efferent nerves.

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The central cough center coordinates what actions to produce a cough?

Deep inspiration
Closure of glottis
Forceful contraction of the muscles of the chest wall, abdomen and diaphragm

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What are the oral antitussives?

Opioids (Codeine, Hydrocodone)
Dextromethorphan (Robitussin, Delsym)
Non-Opioids (Benzonatate)
Antihistamines (Diphenhydramine, Promethazine, Chllorpheniramine, Brompheniramine)

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What is the opioids MOA?

Mu agonist on medullary cough center and respiratory tract.

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What is the dextromethorphan MOA?

Sigma agonist on medullary cough center.

N-methyl-D-Aspartate (NMDA) receptor antagonist on medullary cough center.

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What is the antihistamines MOA?

H1 inverse agonist and muscarinic antagonist on medullary cough center and respiratory tract.

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What is the benzonatate MOA?

Sodium channel blocker

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What is the pharmacological effect of opioid derivatives and antihistamines?

Depresses the cough center
Decreases the sensitivity of the sensory receptors in the respiratory tract.
Dries the respiratory tract.

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What is the pharmacological effect on Non-opioid derivatives (Benzonatate)?

Anesthetizes the sensory receptors in the respiratory tract.
Hypothetically, depresses the transmission of the cough impulses (cannot really change the rate of signal going through the cough center)

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What are the side effects of codeine and hydrocodone?

Nausea, drowsiness, sedation, dizziness and constipation
High addiction and tolerance potential.
Analgesic activity.
*Constipation usually occurs when you are taking it for pain in which the dose is higher.

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What are the side effects of Dextromethorphan?

Nausea, drowsiness, sedation, dizziness, and constipation.
No analgesic activity, sedation, respiratory depression or addiction at therapeutic doses.
Extremely large doses do produce intoxication with hallucinations (out of body experience - must give a very high dose)

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What are the side effects of benzonatate?

Drowsiness, headache, dizziness, nasal congestion, a vague “CHILLY” feeling
*Local anesthetic. Do not break open these pearls - numbness of the lips, tongue, throat - can lead to asphyxia. Works locally, does not affect the CNS.

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What are the side effects of diphenhydramine and promethazine?

Sedation

Anticholinergic effects - decreased secretions.

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What are the topical antitussives?

Local Anesthetics (Robitussin cough drops - menthol and eucalyptus oil, Cepastat Maximum Strength)
Demulcents (Pectin - luden's, halls, Glycerin, Honey, Syrup)

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What is a eutectic mixture?

Two solids together turns into a liquid.

Ex: Camphor and menthol

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What is the MOA of local anesthetics effect of aromatic vapors?

Block NA channels at sensory receptors.

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What is the MOA of demulcents?

Coat and relieves irritation of throat.

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What is the placebo effect’s MOA?

Mom’s touch

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What are the side effects of topical antitussives (local anesthetics and demulcents)?

Irritation, redness, or blistering of skin

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What are the toxicities of topical antitussives?

2 g dose of menthol can be fatal
Concentrations greater than 10% of camphor can produce seizures.
4 teaspoons of 5% camphor can be lethal in children

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What is the MOA of expectorates (guaifenesin)?

Increases mucociliary transport (cilia beat to move the mucus up to the larynx - swallow or spit it out)
Increases the volume of pulmonary secretions

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What are the side effects of expectorates?

N/V, dizziness, headache, rash (fairly inert)

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What are the mucolytics?

Acetylcysteine (Mucomyst and Mucosil)
DNAse (dornase alfa, Pulmozyme)
Water

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What is the MOA of Cetylcyteine?

Free sulfhydryl groups reduce the disulfide bonds (smell) of the mucoproteins and they break apart.

What is the MOA of DNAse?

Deoxyribonuclease (DNA) enzyme. Purulent mucus is composed of highly polymerized DNA. Dornase selectively cleaves DNA thus reducing mucous viscosity.

What it the MOA of water?

Thins mucus by dilution. Must be clean to eliminate bacterial growth cause it could cause severe lung infection

What are the side effects of Acetylcysteine?

Nausea, vomiting Severe rhinorrhea Drowsiness Rare hypersensitivity

What are the side effects of DNAse?

Cough (45% in children) Fever (35%) Rhinorrhea (30%) Voice alteration (20%)

What would you recommend to someone with a cold?

Antihistamine and decongestant

What would you recommend to someone with a virus?

NSAIDs

What would you recommend to someone with bronchitis?

Codeine and dextromethorphan

What would you recommend to someone with non-specific, productive cough?

Guaifenesin

What would you recommend to someone with non-productive cough/ pharyngeal irritation?

local anesthetics and demulcents.

Antitussives slow the transduction of nerve signals through afferent and efferent nerves. T/F

False

Mucolytics thin mucus allowing for easier removal from the lungs. T/F

True

All oral antitussives depress the cough center. T/F

False - benzonatate does not get into the brain to change the cough center.

Dextromethorphan and benzonatate can be addicting. T/F

False

Expectorates ease the removal of mucus from the lungs. T/F

True

What are eicosanoids?

Prostaglandins/Prostacyclins/thromboxanes/Leukotrienes

What are prostaglandins?

Fever/Pain/Inflammatory mediators

What are antipyretics?

An agent that reduces fever by decreasing the mediator prostaglandins responsible for elevating the hypothalamic set-point for temperature control in fever.

What are analgesics?

an agent that reduces pain e.g. via decreased prostaglandins.

What are anti-inflammatorys?

decreased vasodilator prostaglandins (PGE, PGI), indirectly, less edema. Inhibition of adhesion molecule activity. Decreased accumulation of inflammatory cells.

What are NSAIDs?

Non-Steroidal Anti-Inflammatory Drugs : Aspirin, Ibuprofen, Naproxen, etc.

What are COX?

cyclooxygenase enzymes | 3 isoforms: COX-1, COX-2, COX-3

What are LOX?

Lipooxygenase enzyme

What are the mediators of inflammation?

Vasoactive amines (Histamine, Serotonin) Leukocyte products ( ROS + free radicals, lysosomal enzymes) Platelet activating factor (PAF) Cytokines: IL-1, TNF (pyrogens) Chemokines (chemo-attractants) Nitric oxide (NO) Ecosanoids (Arachidonic Acid metabolites) - Prostaglandins

What are the products of arachidonic acid?

Prostaglandins; thromboxanes; prostacyclins; leukotrienes

What enzymes always play a role in arachidonic acid formation?

PLA2 COX-1 (constitutive isoform - always expressed, part of homeostasis) COX-2 ( inducible - signal) COX-3 LOX or 5-lipoxygenase - involved in leukotrienes

Prostaglandins can mediate what types of effects?

``` Inflammation Pain Fever decreased acid secretion in stomach increased alkaline intestinal mucus and HCO3 secretion regulation of blood pressure blood coagulation Uterine contraction ETC. ```

NSAIDs block COX-1 and COX-2 receptors doing what?

Blocking the ability to make different prostaglandins

If you block the LOX then you can't make what?

Leukotienes.

What is the structure of eicosanoids?

Contain 20 C's (ecosane) | named based on the number of double bonds present - can have up to three double bonds.

The eicosanoid PGG3 contains what ring head and how many double bonds?

contains G ring head and 3 double bonds

Where are the double bonds located on PG's?

PG1 (C13/14) PG2 (C13/14 and C5/C6) PG3 (C13/14 and C5/C6 and C17/C18)

What is the most common ARA in humans?

ARA2

Why do we take into account ARA when discussing Fever pain and inflammation? A. Because it potentially inhibits COX enzymes. B. Because it is the PG precursor molecule. C. Because ARA is a key saturated PG molecule. D. Because its formation is enhanced by NSAIDs

B. Because it is the PG precursor molecule.

Your understanding of PG nomenclature is that a theorectical PGJ5 implies...

The PG head ring type is J

What is N-acetyl-para-amino henol?

APAP

What are examples of propionic acids?

Ibuprofen and naproxen

What are the Non-NSAIDs?

``` Anilines or p-aminophenols APAP Acetanilide * Phenacetin * *No longer used due to toxicity ```

What are the salicylates?

``` Aspirin Salicylamide Salicylate salts Salsalate Diflunisal ```

What are the types of Aryl-heteroarylalkanoic acids?

``` Acetic Acids (diclofenac, Etodolac) Propionic acids (Ibuprofen, Naproxen) ```

What are arylanthranilic acids?

Mefainic acid | mechlofenamate Na

What are oxicams?

piroxicacm | meloxicam

What are naphthylakanone?

nabumentone

What are Coxibs?

celebrex

What is the active ingredient of paracetamol?

acetaminophen

What functional group does acetaminophen lack that causes it to not have anti-inflammatory properties?

COOH FG This also is why it does not cause GI toxicity like aspirin

What can be metabolized into APAP using CYP1A2 enzymes?

Acetanilide | Phenacetin

What are the uses of anilines or p-aminophenols and how do they work?

APAP Analgesia is achieved by elevating pain threshold Antipyretic effects require CNS/BBB penetration CNS driven

What increases the toxicity in APAP?

O-methylation and propylation | Ethylation as in APAP decreases toxicity.

Lecture 3 Flashcards

(73 cards)