Lecture 11- Over the Counter Drugs - Cough and Cold

Question 1

What are the 3 classes of drugs involved for cough and cold?

Answer 1

• Antit-tussives
• Decongestants
• Expectorants

Question 2

Commonly avaible OTC cough and cold medication contain either singly or in combination of a ____, ____ , ____ and/or anti____ /____

Answer 2

decongestant; anti-tussive or cough suppressent; expectorant; antipyretic or analgesic

Question 3

What is the most common symptom of upper respiratory tract viral infections?

Answer 3

cough

Question 4

The cough reflex is initiated by the stimualtion of ____ nerves innervating the throat and lungs.

Answer 4

sensory

Question 5

Which receptors do sensory neurons contain that detect irritants and inflammation?

Answer 5

P2X3 and TRPV1

Question 6

Sensory neurons send coughing information to the ____ in the brainstem, medulla oblongata

Answer 6

Nucleus tractis solitarus (nTS)

Question 7

Efferent neurons via ____ and ____ nerves stimulate the diaphragm, intercostal muscles and lungs to initate a cough.

Answer 7

parasympathetic; motor

Question 8

OTC drugs that inhibit the cough reflex do so mostly by inhibiting neurons in the ____.

Answer 8

nTS.

Question 9

____ is a mu opioid receptor agonist.

Answer 9

Opioid

Question 10

mu opioid receptors are located in the ____ as well as peripheral nerves innervating the respiratory tract.

Answer 10

nTS

Question 11

Are opioid receptors inhibitory/excitatory G-protein coupled receptors?

Answer 11

inhibitory (Gi - GPCR)

Question 12

Gi-coupled GPCRs inhibit ____ activity and reduce neuronal activity.

Answer 12

Adenylate cyclase (AC)

Question 13

Activation of opioid receptors inhibit ____ channels, and activate ____ channels and inhibit ____ (AC).

Answer 13

calcium; K+; adenylate cyclase

Question 14

What is the effect on the brain from the inhibition of AC, adenylate cyclase?

Answer 14

reduced neuronal activity and reduced transmitter release.

Question 15

Opioid receptors are also located in the brainstem regions that mediate breathing reflex, in the ____ complex in the medulla oblongata.

Answer 15

Prebotzinger

Question 16

High dose opioids can inhibit the ____ reflex and lead to death.

Answer 16

breathing

Question 17

Codeine is a ____ agonist; it is not very potenet but has high risks.

Answer 17

partial

Question 18

____ is a centrally active NMDA receptor antagonist.

Answer 18

Dextromethorphan

Question 19

What is the effect od dextromethorphan on the brain?

Answer 19

inhibits neurons in the nTS

Question 20

NMDA receptor is a ____ ion channel gated by ____ (excitatory), which leads to neuronal activation.

Answer 20

ligand-gated; glutamate.

Question 21

Dextromethorphan blocks the activation of the ____ receptor and leads to the inhibition of neuronal activation.

Answer 21

NMDA.

Question 22

____ is an antihistamine (H1 inverse agonist)

Answer 22

Diphenhydramine

Question 23

H1 receptors are G____ coupled receptors located on respiratory smooth muscles, stimulate sensory nerves producing coughing.

Answer 23

Gq

Question 24

Diphenhydramine is an inverse agonist meaning it acts as an ____ in the presense of an ____ which is ____.

Answer 24

antagonist; agonist; histamine.

Question 25

Diphenhydramine crosses the ____ to suppress neurons in the ____.

Answer 25

Blood-brain barrier; nTS.

Question 26

What is one of the most effective non-prescription treatment of cough that is not found at the pharmacy?

Answer 26

Honey

Question 27

What are the 3 drugs disccused in the Anti-tussives section?

Answer 27

* Codeine * Dextromethorphan * Diphenhydramine

Question 28

Nasal congestion is due to swelling (____) of the nasal mucosa and edema caused by ____.

Answer 28

edema; vasodilation

Question 29

Does the sympathetic or parasympathetic nervous system control the vasuclar tone?

Answer 29

sympathetic.

Question 30

____ adrenergic receptors are located on vascular arterioles and activation leads to vasoconstriction.

Answer 30

alpha 1

Question 31

____ adrenergic receptors are located on vascular arterioles and veins, and well as broadly throughout the central and peripheral nervous system.

Answer 31

alpha 2

Question 32

____ adrenergic receptors are located on bronchioles (smooth muscle relaxation) and in the heart (increased cardiac output)

Answer 32

Beta

Question 33

Alpha 1 adrenergic receptors are G____ coupled receptors; they convert PIP2 into ____ and ____.

Answer 33

Gq; IP3 and DAG

Question 34

Alpha 2 adrenergic receptors are G____ coupled receptors. They are responsible for the inhibition of adenylate cyclase (AC).

Answer 34

Gi

Question 35

Beta adrenergic receptors are G____ coupled receptors.

Answer 35

Gs.

Question 36

For alpha 1, activation of G____ proteins increase PLC and IP3 pathways. This stimulates release of ____ and smooth muscle ____.

Answer 36

Gq; calcium; contraction.

Question 37

For alpha 2, inhibition of adenylate cyclase reduces ____ which is an inhibitor of myosin light chain kinase, and enzyme that phosphorylates myosin and causes ____. Inhibition of ____ increases MLCK activation and increases smooth muscle ____.

Answer 37

cAMP; contraction; cAMP; contraction.

Question 38

What are sympathomimetic drugs?

Answer 38

drugs that produce effects similar to activation of the sympathetic nervous system.

Question 39

What is the predominent neurotransmitter present in the sympathetic nervous system?

Answer 39

Noradrenaline or norepinephrine.

Question 40

____ is a non-specific agonist at the alpha and beta adrenergic receptors; it is a sympathomimetic drug.

Answer 40

Pseudoephedrine.

Question 41

Pseudoephedrine activates alpha adrenergic receptors in mucosa of the respitaory tract leading to ____ of blood vessels, reducing edema and swelling and opens up nasal passages.

Answer 41

vasoconstriction

Question 42

Pseudoephedrine activity at the beta adrenergic receptors causes ____ ____ ____ leading to dilation of the bronchi and increased mucociliary clearnce helps clear the nasal passage.

Answer 42

smooth muscle relaxation.

Question 43

What are the other effects of Pseudoephedrine?

Answer 43

* shrinks swollen nasal mucous membranes * reduces tissue hypermia * reduces edema and nasal congestion * increases nasal airway latency

Question 44

Pseudoephedrine is structurally related to ____ and has stimulant properties.

Answer 44

Amphetamine

Question 45

____ is a specific alpha 1 adrenergic receptor agonist.

Answer 45

Phenylephrine

Question 46

Phenylephrine leads to vasoconstriction in the nasal mucosa but does not lead to ____ ____ ____ in the bronchi nor does it impact the heart rate.

Answer 46

smooth muscle relaxation

Question 47

____ cannot be chemically transformed into methamphetamine as the structures are different but pseudoephedrine can be transformed.

Answer 47

Phenylephrine

Question 48

____ is an alpha 2 adrenergic agonist.

Answer 48

oxymetazoline.

Question 49

What is the risk with prolonged use of oxymetazoline?

Answer 49

* Can lead to more congestion than it was before; Rhinitis Medicamentosa or rebound congestion.

Question 50

Alpha ____ are restrcited to vascular structures but alpha ____ is not.

Answer 50

1;2

Question 51

Which G-protein coupled receptor is susceptible to rebound signaling?

Answer 51

Gi

Question 52

What are the 3 drugs discussed in the section of Decongestants?

Answer 52

* Pseudoephedrine * Phenylephrine * Oxymetazoline

Question 53

What is the one drug disscused for expectorants?

Answer 53

Guaifenisin also known as mucinex

Question 54

Guaifenesin increases the output of bronchial secretions by by decreasing the ____ and ____ (facilitates expulsion via the cough relfex, makes it less sticky.

Answer 54

adhesiveness and surface tension