Lecture 11- Over the Counter Drugs - Cough and Cold Flashcards

1
Q

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

A
  • Antit-tussives
  • Decongestants
  • Expectorants
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2
Q

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

A

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

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3
Q

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

A

cough

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4
Q

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

A

sensory

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5
Q

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

A

P2X3 and TRPV1

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6
Q

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

A

Nucleus tractis solitarus (nTS)

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7
Q

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

A

parasympathetic; motor

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8
Q

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

A

nTS.

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9
Q

____ is a mu opioid receptor agonist.

A

Opioid

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10
Q

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

A

nTS

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11
Q

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

A

inhibitory (Gi - GPCR)

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12
Q

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

A

Adenylate cyclase (AC)

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13
Q

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

A

calcium; K+; adenylate cyclase

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14
Q

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

A

reduced neuronal activity and reduced transmitter release.

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15
Q

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

A

Prebotzinger

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16
Q

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

A

breathing

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17
Q

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

A

partial

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18
Q

____ is a centrally active NMDA receptor antagonist.

A

Dextromethorphan

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19
Q

What is the effect od dextromethorphan on the brain?

A

inhibits neurons in the nTS

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20
Q

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

A

ligand-gated; glutamate.

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21
Q

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

A

NMDA.

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22
Q

____ is an antihistamine (H1 inverse agonist)

A

Diphenhydramine

23
Q

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

A

Gq

24
Q

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

A

antagonist; agonist; histamine.

25
Q

Diphenhydramine crosses the ____ to suppress neurons in the ____.

A

Blood-brain barrier; nTS.

26
Q

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

A

Honey

27
Q

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

A
  • Codeine
  • Dextromethorphan
  • Diphenhydramine
28
Q

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

A

edema; vasodilation

29
Q

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

A

sympathetic.

30
Q

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

A

alpha 1

31
Q

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

A

alpha 2

32
Q

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

A

Beta

33
Q

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

A

Gq; IP3 and DAG

34
Q

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

A

Gi

35
Q

Beta adrenergic receptors are G____ coupled receptors.

A

Gs.

36
Q

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

A

Gq; calcium; contraction.

37
Q

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 ____.

A

cAMP; contraction; cAMP; contraction.

38
Q

What are sympathomimetic drugs?

A

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

39
Q

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

A

Noradrenaline or norepinephrine.

40
Q

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

A

Pseudoephedrine.

41
Q

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.

A

vasoconstriction

42
Q

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

A

smooth muscle relaxation.

43
Q

What are the other effects of Pseudoephedrine?

A
  • shrinks swollen nasal mucous membranes
  • reduces tissue hypermia
  • reduces edema and nasal congestion
  • increases nasal airway latency
44
Q

Pseudoephedrine is structurally related to ____ and has stimulant properties.

A

Amphetamine

45
Q

____ is a specific alpha 1 adrenergic receptor agonist.

A

Phenylephrine

46
Q

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

A

smooth muscle relaxation

47
Q

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

A

Phenylephrine

48
Q

____ is an alpha 2 adrenergic agonist.

A

oxymetazoline.

49
Q

What is the risk with prolonged use of oxymetazoline?

A
  • Can lead to more congestion than it was before; Rhinitis Medicamentosa or rebound congestion.
50
Q

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

A

1;2

51
Q

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

A

Gi

52
Q

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

A
  • Pseudoephedrine
  • Phenylephrine
  • Oxymetazoline
53
Q

What is the one drug disscused for expectorants?

A

Guaifenisin also known as mucinex

54
Q

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

A

adhesiveness and surface tension