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Misoprostol

cytoprotective

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Epoprosterol

hypertension

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Dinoprostone

termination of pregnancy

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Alprostadil

Erectile dysfunction

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• Mu receptor

• Kappa receptor

Both Mu and Kappa receptors are Gi/Go couple receptors.

Opioid receptors mediating analgesia:

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furan ring

Opioid Analgesics / Narcotic Analgesics

- Removal of this part of structure increase its lipophilicity

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Fatal respiratory depression

common ADR from opiods PHENANTHRENE TYPE ABCDE

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Buprenorphine (Phenan. type)

○ partial mu agonist

○ does not produce

dependence-promoting euphoria

○ may use to slowing down

addiction on morphine

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Nalbuphine (Phenan. type)

○ kappa agonist/mu antagonist

○ mainly used for post-operative/obstetrical anesthesia

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Levorphanol

Butorphanol

Morphinan-Types:

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Levorphanol

○ Mu agonist

○ 4-8x more potent than morphine

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Butorphanol

○ Kappa agonist/mu antagonist

○ 5x more potent than morphine

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Fentanyl

○ 80x more potent than morphine

○ Commonly used for cancer pain

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Meperidine - Phenylpiperidine

○ 0.1x more potent than morphine

○ may cause serious hypotension and neurotoxicity

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normeperidine

Meperidine Toxic metabolite:

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Tramadol

Methadone

Non-phenylpiperidine agents

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Methadone

used for addiction recovery

Manages withdrawal symptoms

best (More addictive, more withdrawal symptoms)

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COX-1

a PG responsible for housekeeping and maintenance functions like activating platelets and acts as a gastroprotective

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opioid derived antidiarrheals

amide/cyanide modification eliminates CNS effects

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Opioid antagonist

acts as a competitive inhibitor at the μ receptor

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Naloxone

adjunct for opioid addiction recovery

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Naltrexone

reverses life-threatening opioid

overdose

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isoleucin

cox 1 sidechain

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valine

cox 2 sidechain

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COX-2

- kasi yung gusto lang natin si COX-1 (good sister). Kapag ininhibit ng NSAID yung COX, the arachidonic acid goes to the LOX na nagccause ng bronchodilation

what does NSAID inhibit

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COX-1 and COX-2

pain and fever responses (they signal the body that there is an inflammation, pain and fever

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liver

Most COX targets __

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Acetylsalicylic acid

that's why aspirin can result to bleeding and ulcers since it irreversibly binds COX-1 (usual | high dosing - including COX-2)

Only irreversible COX-1 inhibitor

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Diflunisal

Non-selective NSAID

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Meclofenamic acid

○ Fenamate NSAID

○ 25x more potent

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TIDES:

Tolmetin

Indomethacin

Diclofenac

Etodolac

Sulindac

Arylacetic acid:

TIDES

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binds the -SH moiety and inhibits lysosomal enzymes responsible for inflammatory responses

Disease-Modifying Anti-Rheumatic Drugs (DMARDs)

MOA:

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active gold (Au+)

DMARDS contains __ essential for binding

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monosodium urate monohydrate crystals

Gout is a joint inflammation due to accumulation of uric acid or ___ in the synovial fluid

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xanthine oxidase inhibitors

uricosurics

recombinant uricases

- attacks the causative agent (uric

acid) by the reducing its amounts

Chronic Gout - you need __ inhibitor

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false.

Chronic - attacks the causative agent (uric

acid) by the reducing its amounts

Acute - colchicine; prevents microtubule polymerization

= reduce microtubule-based inflammation

TOF. Chronic Gout drugs prevents microtubule polymerization

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xanthine oxidase inhibitors

inhibits the production of uric

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uricosurics

areterm-80 agents that promote the

urination of uric acids (tutunaw sa namuong crystals(

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Recombinant uricase

enzymes that can

breakdown uric acid

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colchicine

to remove deposit (nagsstart na magcrystal in acute gout) give:

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purines

Uric acids comes from _

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Alluoporinol

xanthine oxidase inhibitor

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non purine XO inhihibit

non purine XO inhihibit

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Allopurinol

Famous drug for chronic gout

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Probenecid

uricosuric agent

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Colchicine

○ Anti-tubular

○ Acute gout

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Febuxostat

Non-purine XO inhibitor

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chronic bronchitis

emphysema

Common COPD

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○ Beta-2 adrenergic agonists

○ Antimuscarinic agents

○ Methylxanthines

If you want relievers to relieve the symptoms you're experiencing, use:

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○ Mast Cell Degranulation Inhibitors

○ Adrenocorticoids

○ Leukotriene Modifiers

○ Monoclonal Anti-IgE Antibody

○ Phosphodiesterase-4 Inhibitors

If you want to control the possibility of such conditions, use controllers such as:

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Beta-2 agonists (phenylethylamines - PEAs)

terbutaline, salbutamol, pirbuterol

SABA (relief drugs:)

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control of inflammation

main goal of therapy in CHRONIC ASTHMA:

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● Mast cell stabilizers ("crom-")

● PDE Inhibitors (methylxanthines, roflumilast)

● Steroids/glucocorticoids

● Leukotriene antagonists (-lukasts, zileuton)

● Monoclonal anti-IgE antibody therapy

(omalizumab)

Drugs for Chronic Asthma

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TRUE

Asthma can be reversed. TOF

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spasmogens

Mast Cell inhibits the release of bronchial ___ (histidine, LTs, PGs) from sensitized mast cells (bound to IgE).

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furan (khelin)

piperidone ring (nedocromil)

what maintains the activity in chromone

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Methylxanthines (theophylline)

Roflumilast

Phosphodiesters (PDE) Inhibitors

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dialkoxyphenyl ring

Roflumilast has what ring?

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xanthine oxidase

theophylline metabolism

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Theophylline

naturally occurring○ No clear SAR but it is scientifically

proven that it also targets PDE

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lipocortin

Adrenocortids (Glucocorticoids) stimulates synthesis of __

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pregnane ring skeleton must be trans-conformation

Adrenocortids (Glucocorticoids) drugs should have __conformation

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- Antagonize LT receptor (Montelukast, Zafirlukast)

- inhibits the 5- lipoxygenase (Zileuton) resulting in decreased synthesis of LTs.

Leukotriene Modifiers MOA

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Montelukast

● __ Quinoline derivative

mimics triene moiety of LTs = essential for activity

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Zileuton

● Classified as N-hydroxyurea

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N-OH

Zileuton - what is essential for its activity

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Benzothienyl ring

It increases lipophilicity in Zileuton

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5-HT1B and 5-HT1D receptors

"-TRIPTANS" stimulates ___ and __ receptors

- Leads to vasoconstriction = inhibition of

pain stimuli in vessels and nerve

endings in the brain.

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migraines and cluster headaches

"-TRIPTANS" used for

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High blood pressure

SIDE EFFECT of "-Triptans"

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"-SETRONS"

Gold standard for chemotherapy and radiation-induced nausea and vomiting.

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"-setrons"

They mimic serotonin

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Sumatriptan

Prototype -triptan agent

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Rizatriptan

Special because it is prescribed for pediatric migraine

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Granisetron

Antiemetic that is commonly prescribed to chemotherapy patients

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Alosetron

Anti-diarrheal IBS (irritable bowel syndrome)

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Ergotamine

For migraine headache

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Ergonovine

Aids in controlling bleeding from

labor

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Lysergic Acid Diethylamide (LSD)

○ Commonly derived from mushrooms

○ Never been used

○ Literally addictive hallucinogen

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Histaminergic Agents

those that works on histamine receptors and results in different pharmacologic uses (depending on which histamine receptor is being targeted)

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mast cells and basophils

Histamine is commonly found in __ and __ in the body

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- H1-blockers (1st and 2nd generation)

- H2-blocker

Histaminergic Agents

Classes:

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Cationic amine

responsible for receptor binding at the anionic site

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2-3c

The spacer that divides the aromatic moieties and amino group should be __ carbons in length

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remember

bulkier ring = cis- aromatic moiety (can be substituted)

less bulky = trans- aromatic moiety (must be unsubstituted)

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LOX or COX

Eicosanoids is metabolized by __

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PG

affects inflammation, renal function, provides gastroprotection, and increase aqueous humor

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LT

affects bronchoconstriction

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Misoprostol= cytoprotective

Epoprosterol= hypertension

Dinoprostone= termination of pregnancy

Alprostadil= Erectile dysfunction

Latanaprost= glaucoma

MEDAL

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Latanaprost

prostaglandin used for glaucoma

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Analgesic

drugs which provides a relief from pain.

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Opioid Analgesics

naturally occurring opium alkaloid from the latex of opium plants (Papaver somniferum).

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false. no euphoria = less addictive stimulation

TOF. Kappa receptor stimulation results to decreased cAMP and Ca+2 → euphoria — may result to addiction and dependence.

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Pure Antagonist

blocks all activity at both receptor sites with highest affinity to mu receptors

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Agonist/Antagonist

produce potent analgesia at kappa receptor but has strong antagonist activity at mu

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Pure Agonist (full/partial)

acts on the mu receptor; produce potent analgesia with ADRs similar to morphine use

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Opioid Analgesics / Narcotic Analgesics

Substances that possess "morphine-like" effects

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4-phenylpiperidine max of 5 rings

Opioid Analgesics / Narcotic Analgesics

SAR: __ phenylpiperidine

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Codeine and Oxycodone

Opioid known to cause fatal cardiotoxicity in prolonged use

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4-phenylpiperidine

morphine has ___ structure that must contain mx 5 rings

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