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POST-LEC Q&A B2024: AUTACOIDS

1. Ranitidine is a drug used HISTAMINE ANTAGONISTS


for this condition through
antagonism of H2 receptors H1 ANTAGONISTS
at the gastric parietal cells 1ST (OLD) GENERATION 2ND (NEW) GENERATION
PUD/GERD
Brompheniramine, Buclizine, Acrivastine, Cetirizine,
Hydroxyzine, Azatidine, Loratadine,Fexofenadine, Bilastine
Ketotifen, Diphenhydramine,
Promethazine, etc

more sedating (more more anti-inflammatory, higher MW,


lipid-soluble + more affinity for longer duration
cerebral H1), more
anticholinergic

● sedation = most especially in Loratadine


● antiparkinsonism (suppression of extrapyramidal sx → pxs on
antipsychotics = most especially in Diphenhydramine)
● antimuscarinic → antinausea/antiemetic
● adrenoceptor blocking (high HR, low BP)
● 5HT blocking
● local anesthesia (blocks Na+ channels)

H2 ANTAGONISTS

● -TIDINE
● reduces gastric acid secretion via indirect pathway (GERD, Peptic
Ulcer Disease, prevention of bleeding from gastritis, premed for
radio-contrast)

H3 = sleep/cognitive disorders, H4 = chronic anti-inflammatory (asthma)

2. A drug used for treatment DIPHENHYDRAMINE


for allergic reactions. It has
an IV formulation ● 1H antagonist (1st gen blocks Na channels → local anes)
● antinausea/antiemetic, local anesthesia
Diphenhydramine ● anti-parkinsonism → tx of extrapyramidal sx
● sedation

Antihistamines (general): for allergic rhinitis, allergic conjunctivitis, 2nd line


for allergic rhinitis or hay fever (1st is glucocorticoids), atopic dermatitis, 2nd
line for anaphylaxis (1st is Epi), NOT EFFECTIVE IN ASTHMA, sedation,
motion sickness & vestibular disturbances, common cold & cough,
extrapyramidal sx, appetite stimulant, local anesthetic

3. The receptor of LEUKOTRIENE INHIBITORS


montelukast that is blocked
for the treatment of asthma Zileuton 5-LOX inhibitor

Cyst LT1 Receptor to improve asthma CONTROL (inhibits AA conversion to 5-HPETE


and to LTA4)

Monte-LUKAST LTD4 antagonist

reduce FREQUENCY of asthma (competes for CystLT1)


exacerbation

4. Dinoprostone is a drug “”PROST””ANOID RECEPTOR AGONISTS "MADEL"


used for this indication by
acting as an agonist in the EP MisoPROSTol cytoprotective for peptic ulcer;
and FP receptors 'terminates pregnancy'
PGE1
Indication: used for cervical AlPROSTadil patent ductus arteriosus (PDA)/cyanotic
ripening during labor CHD, erectile dysfunction

PGE2 & DinoPROSTone INDUCE LABOR FOR MISSED ABORTIONS


PGF2a & H.MOLE, RIPENING OF CERVIX

PGI2 EpoPROSTenol Vasodilation, HTN

PGF2a LatanoPROST Smooth muscle reLAxant, Open angle


gLAucoma

Si Mis at Din ay binuntis ni Al pero nilaglag ni Mis pak ganon basta maka1 pt

5. The receptor of 5HT AGONIST: Buspirone, Triptans, LOCA/DEX, Tegaserod/Cisa


ondansetron that acts as an
antagonist for treatment of BUSPIRONE (5HT) 1A (neuronal Anxiolytic
vomiting postsurgically inhibition)

5HT3 receptor -TRIPTANS 1B & 1D Acute migraine


(vasoconstriction) (causes cerebral
vasoconstriction)

LOCASERIN/DEXFENFL 2C (appetite Obesity


URAMINE suppression)
LOCA/DEX

TEGASEROD/CISAPRID 4 (tega serod si cisa) GERD


E
5HT ANTAGONIST: Serin/Setron + Cyproheptadine

Cyproheptadine Postgastrectomy Dumping Syndrome,


(peristalsis & Muscle spasms (SC injury), appetite
satiety) (5HT) 2 stimulant

RITANserin Vasospastic
(constriction)

KETANserin HTN, Carcinoid

-SETRON 3 N/V from surgery & cancer

6. A drug that acts as an Ergot Alkaloids: AGONISTS of alpha-adreno, Dopamine, 5HT2


agonist to the 5HT2
receptors used for the BROMOCRIPTINE alpha-adreno + Prolactinemia (high
treatment of migraine. It is dopamine dopamine, low PRL)
an ergot derivative

Ergotamine ErgoNOvine alpha-adreno + 5HT2 for uterine bleeding


(NO pregnant px)

ERGOTamine 5HT2 migraine, induces


cerebral vasoconstri

LSD Dopamine

7. The mechanism by which ASA as an IRREVERSIBLE COX 1 & 2 inhibitor


high dose aspirin exerts its
analgesic and ● daily LOW DOSE: cardioprotective
anti-inflammatory effect ● HIGH DOSE: anti-inflamm & analgesic

Inhibition of COX1 and COX 2 APAP as a weak inhibitor of COX


enzymes COX 1 inh causes GI disturbances

COX 2 inh: E >L=R> Coxib


8. ErgoNOvine is used for tx ErgoNOvine: NO to pregnant women because it is for postpartum bleeding
of this medical situation by
acting as an agonist at the
5HT2 and alpha 1 receptors

Post-partum bleeding

9. A topical drug that is used E: Miso + Al (red)


to treat open angle
gLAucoma and acts as an F: La (yellow)
agonist to the FP receptor E&F: Dino (orange)
LAtanoprost I: Epo

MisoPROSTol

PGE1
AlPROSTadil

PGE2 & PGF2a DinoPROSTone

PGI2 EpoPROSTenol

PGF2a LatanoPROST

10. The mechanism by which ACEI: -pril, ARB: -sartan (no cough)
Enalapril is used for HTN

Inhibition of ACE

11. The receptor of E: Miso + Al (red)


EpoPROSTenol where it acts
F: La (yellow)
as an agonist for tx of E&F: Dino (orange)
pulmonary HTN
I: Epo
IP receptor
MisoPROSTol

PGE1
AlPROSTadil

PGE2 & PGF2a DinoPROSTone

PGI2 EpoPROSTenol

PGF2a LatanoPROST

12. A drug that has E >L=R> Coxib


anti-inflammatory and
analgesic that acts on the
COX2 enzyme inhibitor

COX2 inhibitors (-COXIB)

13. Ibuprofen is a drug used NSAIDS: Ibuprofen, naproxen, indomethacin, piroxicam, mefenamate,
to treat this clinical nabumetone (greatest COX-2 selectivity), KETOROLAC FOR POSTSURGICAL
manifestation by inhibiting ANALGESIA
COX1 and COX2 enzymes

Anti-inflammatory/analgesic

14. The mechanism by which E: Miso + Al


Alprostadil exerts its effect on
the EP receptor to maintain F: La
the PDA in newborns E&F: Dino
Agonism I: Epo

15. The receptor of 5HT Agonist


SumaTRIPTAN where it acts
as an agonist for tx of ● Buspirone = 5HT1A anxiolytic
migraine headache ● TRIPTAN = 5HT1B/1D migraine
● Loca/Dex = 5HT2C obesity
5HT 1D/1B ● Tegaserod/Cisa = 5HT4 GERD

16. A drug that is an agonist 5HT2 Antagonist


to the 5HT1A receptor used
● KetanSERIN = 5HT2 HTN
as an anxiolytic
● RitanSERIN = 5HT2 vasospastic
Buspirone ● Cyproheptadine = 5HT2 Postgastrectomy Dumping Syndrome, Muscle
spasms (SC injury), appetite stimulant
● -SETRON = 5HT3 post-surgical N/V

17. The mechanism by which H1 ANTAGONIST


the drug meclizine is used for
tx of motion sickness ● sedation = most especially in Loratadine
● antiparkinsonism (suppression of extrapyramidal sx → pxs on
antagonist to the muscarinic antipsychotics = most especially in Diphenhydramine)
receptor ● antimuscarinic → antinausea/antiemetic*
● adrenoceptor blocking (high HR, low BP)
● 5HT blocking
● local anesthesia (blocks Na+ channels)

*Scopolamine (antimuscarinic) and H1 antagonists (but less effective if given


during): Diphenhydramine, Promethazine, Piperazines, Cyclizine, Meclizine

18. It is one of the receptors 5HT2 Antagonist


of cyproheptadine, a 1st
generation antihistamine that ● KetanSERIN = 5HT2 HTN
causes increase in appetite ● RitanSERIN = 5HT2 vasospastic
● Cyproheptadine = 5HT2 Postgastrectomy Dumping Syndrome, Muscle
5HT2 receptor spasms (SC injury), appetite stimulant
● -SETRON = 5HT3 post-surgical N/V

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