Pulm and Analgesic Exam 4 Pharm Flashcards by Anton Crepinsek

How do histamine and LT receptors initiate SM contraction?

They are GPCRs that activate Phospholipase C and leads to Ca2+ influx and cGMP to initiate SM contraction

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How do Gq proteins influence the SM in airways?

They activate PLC leading to inc in IP3 and Ca2+ influx resulting in actin/myosin coupling = bronchoconstriction

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How do the Gi proteins influence the SM in airways?

Dec adenylate cyclase activity and cAMP levels = bronchoconstriction (M2)

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How do the Gs proteins influence the SM in airways?

Inc Adenylate cyclase activity and cAMP levels leading to the dissolution of actin/myosin = bronchodilation

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What is the MOA of the Sympathomimetics?

They act via Gs and inc cAMP to relax SM and dec Mast cell degranulation

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What are the impt Sympathomimetics for pulm?

Isoproterenol, albuterol, terbutaline, metaproterenol

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What is one potential problem w/ beta-adrenergic agents?

They can vasodilate in lungs and perfuse poorly ventilated areas; give O2 to counter this effect

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What are the long acting beta-agonists?

Salmeterol and Formoterol

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What are the Methylxantines and their MOA?

Theophylline, Caffeine, Theobromine inc cAMP by preventing breakdown by inhibiting phosphodiesterase

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Who should avoid methylxantines?

Elderly w/ heart conditions

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How do you avoid toxicity of theophylline?

Closely monitor blood levels

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What is the effect of tri-nucleotides on Mast cells?

Inc. GTP stimulate secretion; Inc ATP inhibits secretion

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What is omalizumab?

It is a monoclonal antibody that targets the FC portion of IgE so can’t attach to Fcepsilon

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When do you use chromolyn sodium?

Phophylactically to inhibit asthma exacerbations

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What is the MOA of Zileuton?

It inhibits 5-lipoxygenase to inhibit LT production

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What are the LTD4 receptor antagonists?

Zafirlukast and Montelukast

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When are Leukotriene modifiers especially useful?

Aspirin induced asthma

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What is useful w/ inhaled corticosteroids?

They don’t turn off the rest of the immune system

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What is a risk of rapid withdrawl of corticosteroids

adrenal insufficiency

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Which is special about ciclesonide?

It is designed to be cleaved by esterase locally

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What is a unique risk of inhaled corticosteroids?

Oropharyngeal candidiasis

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What are three benefits of airway delivery?

Speeds delivery of active cmpds 2. Delivers medication to appropriate site 3. Minimizes systemic Side Effects

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What Abx can be used w/ corticosteroids for acute exacerbations?

Doxy

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What receptor is targeted by Antihistamines?

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What are 2 important decongestants and their MOA?

Pseudoephedrine and phenylephrine; alpha adrenergic stimulation

What type of pain is associated w/ breakthrough spikes?

Cancer Pain (compression)

What are Tx options for multiple sclerosis?

IFN-beta, Glatiramer actetate, corticosteroids

How does IFN-beta MOA in MS?

Reduce BBB penetration of immune cells

What drugs can be used as abortive tx of migraines?

Acetaminophen + Caffeine, Triptans, Ergotamine they all cause vasoconstrictions

What drugs can be used for migraine prevention?

Antidepressants, anti-seizures, and beta-blockers

Describe Abeta fibers

Non-noxious (touch and pressure) and Fastest

Describe Adelta fibers

Pain, cold; myelinated; Fast; 1st pain reflex arc

Describe C fibers

Pain, Temp, Touch, Pressure, Itch; Unmyelinated and slow

Where do Adelta fibers terminate?

Lamina 1

Where do C fibers terminate?

Lamina 2

What is central sensitization?

It is an enhanced activity of the glutamate system

What are the 2 types of alkaloids that Opium contains?

Phenanthrenes and Benzylisopuinolines

What are the Phenanthrenes?

Morphine, Codeine, and Thebaine

What are the Benzylisopuinolines?

Noscapine and Papaverine

What determines the antagonist quality of the Phenanthrenes?

The bulkiness of the N-allyl group; bulkier = more antagonistic

What does methylation at the 3 position -OH of morphine produced?

Codeine - which has decreased potency

What does ketone formation at the 6th position -OH of morphine give?

Hydromorphone which has an increased activity

What metabolite of morphine is still potent?

Morphine-6-glucuronide

Where are phenanthrenes metabolized?

Liver

How are phenanthrenes excreted?

Glomerular filtration; 90% in 24hrs

What are the opioid receptors and their respective endogenous peptides that activate them the most?

Mu - Endorphins; Kappa - Kynorphins; Delta - Enkephalins; Orphanin Opioid Receptor/Nociceptin - Nociceptin/Orphanin FQ

What is a reason to not use Kappa opioid receptor agonists?

They cause dysphoria

What beta-endorphins act on the Mu-receptor?

Pro-opiomelanocortin (endogenous morphine)

Describe Signal Transduction of the Opioid Receptor

Presynaptically located and is Gi linked to dec cAMP so dec Ca2+ and dec release of NT; also linked to a K+ channel so causes hyperpolarization

Why do you use Hydromorphone post-op?

It is 4-5x more potent than morphine and has a >t1/2 than fentanyl

What drug do you give if they are opioid intolerant?

Meperidine

What receptors are affected by Buprenorphine?

Partial mu agonist, weak Kappa agonist, delta antagonist

What is the use of buprenorphine?

It is used to tx opioid withdrawal

What is the MOA of Tramadol?

It is a 5HT releaser and NE reuptake inhibitor, weak mu opioid agonist

What is 4x as potent as Tramadol

Its O-demthylated metabolite

What is Tapentadol?

A weak mu agonist and inhibits norepi reuptake

How should buprenorphine be administered for opioid misuse?

Oral admin

How should Naloxone be administered for opioid misuse?

IV admin

What are the Arylproprionic Acids?

Ibuprofen and naproxen

What are the Arylacetic acids?

Indomethacin and Diclofenac

What are the Enolic acids?

Piroxicam

What are the p-Aminophenols?

Acetaminophen

Where is COX2 constitutively expressed?

The brain and spinal cord. This is why it is induced in setting of inflammation

Where does ASA affect COX enzymes?

It acetylates Ser529

Where is ASA absorbed?

Jejunum

What is the difference b/w the t1/2 of ASA and Salicylate?

ASA = 15 mins; Salicylate = 12 hrs

How do you inc the excretion of ASA?

Give bicarb to inc the pH of urine. ASA is passively reabsorbed from tubule so if can deprotonate it won't diffuse through membranes

What are the methods of metabolism for nonsalicylate NSAIDs

1. oxidation, 2. Demethylation, 3. Conjugation

What is the major difference b/w ibu and naproxen?

t1/2: Ibu - 2 hrs, Naproxen - 14 hrs

What is the big risk w/ Diclofenac?

Peptic ulcers long term

What is one of the most potent reversible inhibitors of PG synthesis?

Indomethacin

What are the uses of Indomethacin?

Acute gouty arthritis, Ankylosing Spondylitis

What is Sulindac?

Less toxic indomethacin derivative

What are the uses of Sulindac?

RA and Ankylosing Spondylitis

What is the risk of p-Aminophenols?

Acute overdose can lead to fatal hepatic necrosis

How do you tx the gastric SE of salicylates?

Misoprostol a PGE1 analog

What are the affects of Salicylate OD

Metabolic acidosis w/ compensatory respiratory alkalosis

What do you give to tx salicylate OD?

Dextrose, Sodium Bicarbonate to inc urinary excretion

How does Acetominophen damage the kidneys?

It inhibits PGE2 which induces vasoconstriction and results in papillary necrosis

What is Leflunomide and MOA?

It is an antiproliferative agent that initiates G1 arrest to inhibit T-cell proliferation and B cell Ab production

What is Anakinra?

Recombinant IL-1 Receptor antagonist

What are absolute contraindications of anakinra?

Pre-existing malignancy and neutropenia

What are the TNF-alpha blocking agents?

Etanercept, Infliximab, adalimumab

What is Febuxostat?

It is a non-purine inhibitor of Xanthene oxidase

What is the MOA of Probenacid?

It competes for renal tubular anion transporter of uric acid and blocks reabsorption

What are the topical anesthetics that inhbit Na channels?

Lidocaine, Benzocaine, and Oxybuprocaine

What is the difference b/w Lidocaine and Bupivicaine?

Lido lasts 30min-2 hrs and Bupivicaine lasts 3.5 hs

What are the Na channel blockers that are also Tricyclic Antidepressants?

Amitryptiline, Carbamezipine, and Lamotrigine

What is a big risk of Lamotrigine?

Steven-Johnson Syndrome

What enzyme is impt for metabolism of TCA/SNRI?

CYP2D6

Where are TCA/SNRIs excreted?

Renal Excretion

Where are Ca Channels that can be affected in pain tx expressed

Nerve terminals

What are the CCBs for pain tx?

Gabapentin, Pregabalin, Ziconotide, and Levetiracetam

What is Qutenza?

It is used to desensitize a nerve and reduce expression of TRPV1

What is a risk of TRPV1 antagonists?

Hyperthermia b/c of heat intolerance