Anti-hist. / Expectorants/ Mucolytics…

Question 1

ANTI-HISTAMINES: FIRST GENERATION
Exs.

Answer 1

-ine
Examples: diphenhydramine, promethazine,
chlorpheniramine, meclizine, dimenhydrinate,
hydroxyzine

Question 2

-ANTI-HISTAMINES: FIRST GENERATION
MoA

Answer 2

Cross the blood-brain barrier so there are sedative effects

-Mechanism of action: Reversible competitive
antagonists of H1 receptors
- May be ineffective at high levels of histamine

Question 3

Clinical uses of ANTI-HISTAMINES: FIRST GENERATION

Answer 3

 Allergic reactions, rhinitis, urticaria
 Cold medication
 Sleep aid
 Pre-op sedation
 Nausea/vomiting
 Motion sickness, vertigo

Question 4

H1- receptors cause

Answer 4

1. Bronchoconstriction
2. Itching (b/c receptors are activated)
3. Incr. vascular permeability
4. Nasal irritation/sneezing/ congestion
5. Vasodilation

Question 5

ANTI-HISTAMINES: Side effects due to blockade of

Answer 5

 Central nervous system histamine receptors
 Muscarinic receptors
α1-adrenergic receptors

Question 6

ANTI-HISTAMINES: ADVERSE EFFECTS

Answer 6

 Sedation
 Blurred vision
 Dry mouth
 Urinary retention
 Headache

Question 7

ANTI-HISTAMINES: SECOND GENERATION
Exs.

Answer 7

-ine
1. Loratadine
2. Desloratadine
3. Fexofenadine
4. Cetirizine

Question 8

‘ANTI-HISTAMINES: SECOND GENERATION
MoA

Answer 8

• Decreased penetrance into CNS
• Less sedative effects compared to first generation
  (Don’t cross BBB)

Question 9

ANTI-HISTAMINES: SECOND GENERATION
Clinical use+ side effects

Answer 9

Clinical uses: allergy
Side effects: uncommon

Question 10

When are COUGH SUPPRESSANTS used + what’s the MoA

Answer 10

DONT USE TO SUPPRESS COUGH
- Best to treat underlying cause rather than
cough
- Mechanism of action: Ill-defined effect in
brainstem ‘cough center’
-Gi-linked µ-receptors

Question 11

COUGH SUPPRESSANTS
Exs

Answer 11

Opioids: suppress cough in doses below
those required for pain relief
1. Codeine
2. Pholcodeine
3. Morphine

Question 12

Codeine is?

Answer 12

weak opioid
 Less addiction than morphine

Question 13

Pholcodeine is? Is it short or long acting?

Answer 13

has similar but possibly less
intense adverse effects than codeine;
long-acting

Question 14

Morphine is used for…

Answer 14

Palliative care in lung cancer cough
(For analgesia too)

Question 15

OPIOD ADVERSE EFFECTS

Answer 15

 Constipation  Drowsiness  Dry mouth  Miosis  Nausea/vomiting  Respiratory depression

Question 16

Opioid CI

Answer 16

Should be avoided in chronic pulmonary infection
and asthma
- Thickening of mucus and retention
- Risk of respiratory depression

Question 17

COUGH SUPPRESSANTS
Ex.

Answer 17

Dextromethorphan: morphine derivative

Question 18

Dextromethorphan MoA
(Doesn’t act like opioid )

Answer 18

Binds σ receptors
 Also binds serotonergic receptors and inhibits reuptake of serotonin
—>May cause serotonin syndrome if combined with other serotonergic agents
 Effects mediated via opioid receptors only in excess
- Naloxone can be given for O/D
 Also antagonizes glutamate NMDA receptors at higher therapeutic doses

Question 19

Dextromethorphan AE

Answer 19

Uncommon; dizziness, nausea, vomiting,
or GI disturbance
( it’s well tolerated)

Question 20

EXPECTORANT ex. + therapeutic Indication

Answer 20

Guaifenesin is the only FDA-approved expectorant

Therapeutic indication: symptomatic relief of acute
productive cough

Question 21

Guaifenesin MoA

Answer 21

Mechanism of action
 Increases the volume of respiratory secretions
 Decreases the viscosity of bronchial secretions
 Does not suppress the cough reflex

Question 22

Is Guaifenesin used alone?

Answer 22

Used alone or in combination with antihistamines,
cough suppressants, and decongestants

Question 23

DECONGESTANTS exs.

Answer 23

1. Pseudoephedrine
2. Phenylephrine

Question 24

-Pseudoephedrine MoA

Answer 24

a1 adrenergic agonist and release of norepinephrine

-Methamphetamine precursor

Question 25

Pseudoephedrine AE

Answer 25

- not preferred b/c of all the AE CNS stimulation, anxiety, hypertension, urinary retention, tachycardia, nausea/vomiting

Question 26

Phenylephrine MoA

Answer 26

 Selective a1 adrenergic agonist  Less CNS stimulation than pseudoephedrine

Question 27

Classic mucolytic ex.

Answer 27

N-acetyl cysteine used in COPD; cystic fibrosis Evidence of efficacy is poor

Question 28

MUCOLYTICS MoA

Answer 28

 Depolymerizes the mucin glycoprotein oligomers via disulfide bond hydrolysis  Decreases mucus viscosity

Question 29

MUCOLYTICS antidote+ AE

Answer 29

Antidote for paracetamol overdose Side effects: nausea, vomiting, flushing, rash

Question 30

MUCOLYTICS are? + exs.

Answer 30

Secondary polymer network of DNA and F-actin develops in secretions with airway inflammation 1. Peptide mucolytics 2. Hypertonic saline

Question 31

Peptide mucolytics exs.

Answer 31

Dornase alfa (recombinant human DNAse)

Question 32

Dornase alfa MoA + clinical use

Answer 32

Mechanism of action: depolymerizes DNA Used in cystic fibrosis

Question 33

Hypertonic saline (sodium chloride) MoA

Answer 33

Disrupts ionic bonds within the mucus gel Dissociates DNA from mucoproteins allowing natural proteolytic enzymes to digest the mucoprotein