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Pharm > Lecture 7: OTC Cough and Cold > Flashcards

Lecture 7: OTC Cough and Cold Flashcards

1
Q

What do Pharmacological mechanisms of actions fundamentally begin with?

A

A drug receptor interaction

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2
Q

What four types of ingredients do commonly available cough and cold medications contain?

A
  • Decongestants
  • Cough suppressants
  • Expectorants
  • Anti-pyretics
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3
Q

What are OTC cough and cold medications used to treat?

A

Symptoms of upper respiratory infections (runny nose, congestion, cough, fever)

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4
Q

What is the purpose of the coughing reflex?

A

To clear the breathing passage of irritants, microbes, fluids and mucus

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5
Q

What is the function of the mucus in the upper respiratory tract?

A

The mucus is protective. It provides a barrier between the lumen of the airway and the epithelium

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6
Q

Why is mucus upregulated during infection?

A

To prevent penetration of those microbes and to provide substance to clear garbage out of the lungs and airways

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7
Q

Why would it be bad to suppress cough during bacterial infections?

A

Because the cough is used to get that bacteria out

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8
Q

What happens when you cough with viral infections?

A

You end up aerosolizing the particles because they’re so small

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9
Q

What is the coughing reflex initiated by?

A

The stimulation of sensory nerves innervating the throat and lungs

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10
Q

Which receptors in the throat detect irritation?

A

P2X3 and TRPV1

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11
Q

Where do the sensory neurons in the throat that detect irritation send their information?

A

To the cough center in the medulla oblongata

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12
Q

What happens after irritation is sent to the cough center in the medulla?

A

Efferent nerves via parasympathetic and motor nerves stimulate the diaphragm, intercoast muscles and lung to initiate a cough

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13
Q

What is the main nerve that stimulates the cough reflex?

A

CNX the vagus nerve

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14
Q

What are Anti-tussives?

A

OTC drugs that inhibit the cough reflex

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15
Q

How do most anti-tussives work?

A

By inhibiting neurons in the medulla oblongata

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16
Q

What are the three approved anti-tussives?

A
  • Dextromethorphan
  • Diphenhydramine
  • Codeine
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17
Q

What is Codeine in terms of receptors?

A

A mu opioid receptor agonist

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18
Q

Where are Mu opioid receptors located?

A

In the medulla oblongata (cough center) and peripheral nerves innervating the respiratory tract

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19
Q

What is the most abundant opioid receptor in the CNS?

A

Mu

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20
Q

What is meant by codeine is a mu opioid receptor agonist?

A

Codeine activates opioid receptors

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21
Q

What kind of receptors are Opioid receptors?

A

They are inhibitory G-protein coupled receptors (GPCRs)

22
Q

What happens when opioid receptors are activated by Codeine?

A

They inhibit calcium channels, activate K+ channels and inhibits adenylate cyclase which inactivate neurons and reduces neurotransmitter release in the cough center of the medulla

23
Q

Which part of the CNS does Codeine act on?

A

The cough center of the medulla

24
Q

Why are antitussives that contain codeine not recommend for those under 18?

A

Because they have undesirable effects like addiction and overdose. An can inhibit other brain areas like breathing area

25
Q

What is codeine converted to in the CNS?

A

Morphine

26
Q

How does Dextromethorphan work at the receptor?

A

It is a centrally active NMDA receptor antagonist

27
Q

What are NMDA receptors?

A

Ligand gated ion channels gated by glutamate that allow sodium and calcium through and activates neurons

28
Q

Which neurons does Dextromethorphan inhibit?

A

Neurons in the medulla oblongata like codeine

29
Q

What is a brand name of Deztromethorphan?

A

Buckley’s!

30
Q

What are the Pharmacological characteristics of Diphenhydramine?

A

It is an antihistamine (H1 inverse agonist)

31
Q

What kind of receptors of H1 receptors?

A

Gq coupled GPCRs

32
Q

Where are H1 receptors located?

A

On respiratory smooth muscles

33
Q

What do H1 receptors do?

A

They stimulate sensory nerves to produce coughing

34
Q

What does Diphenhydramine do to H1 receptors?

A

It inhibits histamine action at the receptors

35
Q

Besides at H1 receptors how else does Diphenhydramine work?

A

It crosses the BBB to suppress the medullary cough center

36
Q

What is the common decongestant?

A

Pseudoepinephrine

37
Q

What is Pseudoepinephrine?

A

A decongestant

38
Q

What are the pharmacological characteristics of Pseudoephedrine?

A

It is an agonist at the alpha and beta adrenergic receptors

39
Q

What is Pseudoephedrine very similar to?

A

Norepinephrine

40
Q

What is meant by Pseudoephedrine being sympathomimetic?

A

It mimics the effect of Norepinephrine adrenergic receptors

41
Q

What kind of responses does Pseudoephedrine activate?

A

Fight or flight type responses

42
Q

How does Pseudoephedrine affect alpha adrenergic receptors?

A

It leads to vasoconstriction of blood vessels in the respiratory tract causing less mucus release

43
Q

How does Pseudoephedrine affect beta adrenergic receptors?

A

It causes smooth muscle relaxation leading to dilation of the bronchi

44
Q

What is the overall effect of Pseudoephedrine?

A
  • Shrinks swollen nasal mucus membranes
  • reduces tissues hyperemia (blood flow)
  • Reduces edema
  • Reduces nasal congestion
45
Q

What happens if too much of Pseudoephedrine is taken?

A

Because it affects beta adrenergic receptors there will also be heart affects which is an off target effect

46
Q

What is Pseudoephedrine structurally related to?

A

Meth and can be used a precursor to create meth

47
Q

What is different between Pseudoephedrine and Phenylephrine?

A

Phenylephrine is a specific alpha adrenergic receptor agonist

48
Q

What effects will Phenylephrine have?

A

It will cause vasoconstriction of the nasal mucosa but not smooth muscle relaxation

49
Q

What are Expectorants?

A

Oral drugs that enhance the clearance of mucus

50
Q

What is Guaifenesin?

A

An expectorant

51
Q

What does Guaifenesin do?

A

Increases the output of the bronchial secretions by decreasing the adhesiveness and surface tension

52
Q

What is the suggested mechanism of Guaifenesin?

A

It acts as an irritant of gastric vagal receptors that recruit efferent parasympathetic reflexes causing glandular exocytosis that is comprised of a less viscous mucus mixture

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