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PDAT4 > 40 - Pulmonary Medchem > Flashcards

40 - Pulmonary Medchem Flashcards

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1
Q

What Pulmonary Drug Class?

DILATION of Bronchial Passages
Vasodilation in muscle + Liver
Relaxation of uterine muscle // release of insulin
by
AGONISING –>
SYMPATHETIC/Adrenergic Receptors

A
  • *BETA-ADRENERGIC AGONISTS**
  • *-TEROL** / -TERENOL / Terbutaline
  • *B2: Relaxes**

A1: Contracts minor

FROM:
EPINEPHRINE

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2
Q

Beta-Adrenergic Agents

Originate from what Endogenous Compound?

A
  • *CATECHOLAMINES**
  • *Epinephrine / Norepinephrine**

Only the R** **enantiomer = ACTIVE

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3
Q

What are the 3-point interactions for RECEPTOR BINDING

A

EPINEPHRINE

1) Para/Meta -OH

2) Beta -OH

3) -NHR

Metabolism:
MAO / COMT

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4
Q

Beta-Adrenergic Agent Parent Structure:

What is ESSENTIAL for BINDING?

A
  • *1*_ or _2***
  • *AMINO GROUP**

seperated by:
TWO CARBONS

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5
Q

Beta-Adrenergic Agent Parent Structure:

What INCREASES BETA-2 SELECTIVITY?

A
  • *BULKY N-SUBSTITUENT**
  • *N-Tertiary Butyl**

or

Aromatic MethylHydroxy Substitution

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6
Q

Beta-Adrenergic Agent Parent Structure:

What give PROTECTION from MAO?

A

LARGER AMINO SUBSTITUENT

  • *Alpha Carbon Sub**
  • but also decreases alpha/beta activity*
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7
Q

Beta-Adrenergic Agent Parent Structure:

What does a
ALPHA-CARBON SUBSTITUTION
do?

A
  • DECREASED*
  • *Alpha + Beta Activity**
  • BUT*:
  • *MAO PROTECTION**
  • *= longer DOA (drug action) & Oral Bioavailability**
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8
Q

Beta-Adrenergic Agent Parent Structure:

What does the replacement of… do?

CATECHOL –> RESORCINOL

A

Protection from COMT

↑oral BioAvailability

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9
Q

What Drug?

A
  • *ISOPROTERENOL**
  • *Short-Acting B-adrenergic Agonist**

Catechol - Based

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10
Q

Isoproterenol

Drug Type / Metabolism / Disadvantages

A

SHORT ACTING - B2 Adrenergic Agent
Catechol-based

Most POTENT** **bronchodialator

Oxidation Labile –> BENZOCHINONE

  • Disadvantages:*
  • *Cardiac ADR** = NOT B2 specific
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11
Q

Which Drug?

A

ALBUTEROL** / **SALBUTAMOL
SHORT-ACTING- B2 Adrenergic Agents

N-Tertiary Butyl –> B2 Selectivity

Aromatic MethylHydroxy Substitution –> B2 Selectivity

Alpha Substitution –> MAO Protection

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12
Q

What Drug?

A
  • *TERBUTALINE**
  • *Short-Acting B2 Adrenergic Agonist**

Resocinol Based = No COMT Metabolism

N-Tertiary Butyl = ↑B2 Selectivity

  • *Alpha Substitution = MAO PROTECTION**
  • decreased Alpha&Beta Selectivity*
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13
Q

What Drug?

A
  • *METAPROTERENOL**
  • *Short-Acting B2 Adrenergic Agonist**

Resocinol Based = No COMT Metabolism

  • *Alpha Substitution = MAO PROTECTION
  • decreased Alpha&Beta Selectivity***
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14
Q

What are the SHORT ACTING

Beta-Adrenergic Agonists?

A
  • *Isoproterenol**
    0. 5-2 hours

Metaproterenol
3-4 hours

Tertbutaline / Pirbuterol
B2>B1 selectivity, 4-8 hours

Albuterol / Levalbuterol / Salbutamol
B2>B1 selectivity, 4-8 hours

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15
Q

What are the LONG ACTING
Beta Adrenergic Agonists?

A

All orally active –> not metabolized by BOTH COMT nor MAO
>12 hours

Salmeterol
long lipophylic side chain

Formoterol
prodrug

Bambuterol
prodrug

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16
Q

What are the ULTRA LONG ACTING
Beta-Adrenergic Agents?

A

INDACATEROL
Racemate, >24 hours

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17
Q

What Drug?

Study These Flashcards
A
  • *SALMETEROL**
  • *Long-Acting Beta Adrenergic Agonist**

Long Lipophlic Side Chain
racemate

Orally active –> NOT metabolized with MAO nor COMT

18
Q

What Drug?

Study These Flashcards
A
  • *Formoterol / Bambuterol**
  • *Long-Acting Beta Adrenergic Agonist**

BOTH PRODRUGE
Racemate

Orally active –> NOT metabolized with MAO nor COMT

19
Q

What Drug?

Study These Flashcards
A

EPINEPHRINE
(R) = Norepinephrine

  • NON-SELECTIVE B-adrenergic AGONIST*
  • LEAST SELECTIVE*
  • *Used for Allergic Reactions**
  • *Fast action = half life = 2min**
20
Q

Which Pulmonary Drug Class?

*ANTAGONIZES* –> M3 RECEPTOR
VVV
↓cGMP
VVV
DILATE Bronchoconstrictor Muscles
↓Mucus Secetion
VVV
Dilation of Bronchial Passages

Study These Flashcards
A

ANTICHOLINERGICS** = **ANTIMUSCARINIC
BronchoDilator

Tiotropium = LA

Ipatropium = Short Acting

Atropine + Scopolamine

21
Q

What Drugs?

Study These Flashcards
A

Atropine** + **Scopolamine

  • *Anticholinergics = Antimuscarinics**
  • Similar to ACETYLCHOLINE = ACh*

Naturally occuring TROPINE ALKALOIDS

22
Q

Wuz dis?

Study These Flashcards
A

TROPANE

Nitrogenous Bi-Cyclic Compound

hydroxylated –> Tropine

Atropine / Scopolamine
Anticholinergics = Antimuscarinics

23
Q

Wuz Dis?

Study These Flashcards
A

TROPINE

Hydroxylated TROPANE

Esters of TROPINE = Atropine + Scopolamine

24
Q

What Drug?

Study These Flashcards
A
  • *IPATROPIUM**
  • SHORT-ACTING* Anticholinergic

Phenyl Ring = More Likely to be Oxygenated
SHORT ACTING

does NOT diffuse into the BLOOD –> no SYSTEMIC ADRs

  • *QUATENARY AMINE**
  • -> does NOT cross the BBB = no AC ADRs

NON-SELECTIVE Antimuscarinic –> but ONLY M3 in the LUNGS

25
**What Drug?**
* *_TIOTROPIUM_** * *LONG-ACTING Anticholinergic** *does NOT diffuse into the BLOOD* --\> ***no SYSTEMIC ADRs*** * *_QUATENARY AMINE_** - -\> **does NOT cross the BBB** = *no AC ADRs* ***_NON-SELECTIVE_*** **_Antimuscarinic_** --\> but **ONLY M3 in the LUNGS**
26
**What is ESSENTIAL** for ## Footnote **ANTICHOLINERGIC ANTAGONIST = Antimuscarinic** **Tiotropium / Ipatropium**
**_R1**_ _**needs to point BACKWARDS_**
27
**What makes 3 things make** **an** ## Footnote **AntiCholinergic Antigonist** **_MOST POTENT?_**
* *_R1_** **_= AROMATIC_** - -\> VanderWals w receptor * *_R2 = HYDROPHOBIC RING_** * limited size* **_R3 = HYDROGEN BONDING_**
28
**Which Drug type?** * **_Reduce:_*** * *inflammation in airways** * *Lung Damage & airway narrowing** from inflammation * *Mucus Production**
**_CORTICOSTEROIDS_** Based from Cortisol **↑****Expression of _B2 Receptors_** ↑**Upregulates expression of _LIPOCORTIN-1_** --\> ↓***supresses _Phospholipase A2_*** ↓**Expression of *_Pro-Inflammatory Proteins / Cytokines ↓Prostaglandins & Leukotrienes_*** ↓**Supresses** ***_Cyclo-Oxygenase Expression_***
29
**What MoA of CORTICOSTEROIDS** **are INCREASING / UPREGULATING?**
**↑****Expression of _B2 Receptors_** ↑**Upregulates expression of _LIPOCORTIN-1_** --\> ↓*supresses Phospholipase A2*
30
**What MoA of CORTICOSTEROIDS** **are *SUPRESSING / REDUCING?***
* ↑Upregulates expression of LIPOCORTIN-1* - -\> ↓***supresses _Phospholipase A2_*** ↓**Expression of *_Pro-Inflammatory Proteins / Cytokines_*** ***_↓Prostaglandins & Leukotrienes_*** ↓**Supresses** ***_Cyclo-Oxygenase Expression_***
31
**Given that CORTICOSTEROIDS** * *do *_NOT_* act DIRECTLY on the AIRWAY SMOOTH MUSCLE** * do NOT provide immediate relief* **_WHY ARE THEY INHALED?_**
**_AVOIDS FIRST PASS METABOLISM_** so we can use lower doses --\> systemic absorption
32
**What type of Drug?**
**_ORAL = SYSTEMIC CORTICOSTEROIDS_** Anti-Inflammatory Agents
33
**What TYPE of drug?**
**_INHALED CORTICOSTEROIDS_**
34
**Which Leukotriene Modifier?** **Blocks the _SYNTHESIS_ of Leukotriens?**
**_ZILEUTON_** **Inhibits *_5-LIPOXYGENASE_*** *other 2 drugs just block the BINDING*
35
**What drug type?** **Inhibition of \_\_\_\_\_\_\_** VV ***Reduction*** of **Bronchoconstriction & Inflammation** *less effective vs Corticosteroids* w/ **less side effects**
**_LEUKOTRINE MODIFIERS_** _Montelukast / Zafirlukast_ * *LTRA = Leukotriene Receptor Antagonist** * Block action of Leukotriene on the Leukotriene Receptor* * *_Zileuton_** * *Inhibitor of 5-Lipoxygenase**
36
**What drug?**
* *_ZAFIRLUKAST_** * *Leukotrine Receptor Antagonist** = **LTRA** --\> Anti-Inflammatory Agent *Blocks the action of:* **_Leukotriene_ on the Leukotriene Receptor** @ lungs & bronchial tubes, by BINDING to it
37
**What drug?**
* *_MONTELUKAST_** * *Leukotrine Receptor Antagonist** = **LTRA** --\> Anti-Inflammatory Agent *Blocks the action of:* **_Leukotriene D4_ on the Leukotriene Receptor** @ lungs & bronchial tubes, by BINDING to it
38
**What Drug? & MoA?**
* *_THEOPHYLLINE_** * *Methylxanthine** Relaxing effect on Bronchial Smooth Muscle: ***_Competitive NON-selective PD-4 INHIBITOR_*** VV *inhibits* **_Leukotriene Synthesis_** --\> ***Reduces Inflammation***
39
**Which Drug Type?** **Prevent & Control ALLERGIC Disorders** *Blocking of:* **Calcium Channels** essential for **Mast-Cell Degranulation** & **Cell Stabilization** VVV ***_Prevent release of HISTAMINE + Related Mediators_***
* *_MAST CELL STABILIZERS_** * *Chromolyn (Nedocromil) / Chromone** *without intracellular CALCIUM* VV **histamine vesicles CAN'T** **fuse to the cell membrane & degranulate**
40
**Omalizumab = Xolair** Indication / ADR / MoA
For patients with: * *Severe / Persistant ALLERGIC ASTHMA** * that is not controlled with HIGH doses of Corticosteroids* * **_CAUSES ANAPHYLAXIS_*** * does NOT work immediately --\> not for ACUTE* * *SUBQ Inj Q2-4Weeks** **_BINDS TO IgE**_ --\> _***prevents CROSSLINKING*_**

PDAT4 (34 decks)

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