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Pharmacology FINAL (2nd sem) > A: 34-38 > Flashcards

A: 34-38 Flashcards

1
Q

Drugs used in Parkinsons

A
  • Levodopa/Carbidopa- precursor of dopamine
  • Selegeline- MAO-B inhib.
  • Entacapone- COMT inhib. entaCapon for Comt
  • Ropinirole-
    • Dopamine-2 agonist. same ROLE as dopamine
  • Pramipexole-
    • Dopamin 3 agonist
  • Amantadine -
    • Anti-viral
    • M-block
    • enhance dopaminergic transmission ( increase synthesis/release, decrease reuptake)
  • Procyclidine- Ach blocker
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2
Q

Why give Ach blockade in Parkinsons?

A

When physiologic Dopamine decreases –> excessive excitation of cholinergic neurons ( Ach release)

Ach and Dopamine are out of balance in parkinsons

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3
Q

Levodopa/Carbidopa-

MOA ,duration

A

precursor of dopamine

Carbidopa:

  • Dopamine DeCarboxylase inhibitor (periphery)
  • does NOT enter CNS

L-DOPA:

  • prolonged plasma T1/2
  • lower doses of L-dopa is effective
  • fewer peripheral SE

*oral COMT & MAO-B Inhibitors allow smaller doses & prolong action.

  • responsiveness gradually decreases with time
  • DOA= 6-8hrs
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4
Q

Levodopa/Carbidopa-

indication

A

Primary drug used in Parkinsons

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5
Q

Levodopa/Carbidopa-

SE

A
  • GI upset:
  • dyskinesia (on-off phenomenon)
  • behavioral effects:
    • anxiety .
    • hallucination,
    • depression,
    • confusion ,
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6
Q

Dopamine agonists

A
  • Pramipexole
    • D3-agonist
    • IND:
      • monoth. in early parkinsons disease
      • adjunct with L-DOPA in advanced disease
    • oral
    • renal elim
  • Ropinirole
    • D2 agonist
    • IND:
      • monoth. in early parkinsons disease
      • adjunct with L-DOPA in advanced disease
    • oral
    • Hepatic metab
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7
Q

Dopamine agonists side effects and drugs

A
  • pramipexole
  • ropinirole
  1. anorexia
  2. nausea
  3. constipation
  4. postural hypotension
  5. dyskinesia
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8
Q

MAO-I

A
  • selegiline
    • Inhibits MAO-B
    • IND:
      • monoth. in early parkinsons
      • adjunctive with L-DOPA /carbidopa in advanced disease
    • oral
    • long T1/2
    • hepatic metb. to form des-methyl-selegiline (neuroprotective) and amphetamine (psychosimulant)
    • hungarian development!!!!
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9
Q

MAO-I SE

A
  • Serotonin syndrome with
    • meperidine (opioid)
    • SSRI
    • TCA
  • dyskinesia
  • psychosis
  • hypotension
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10
Q

COMT inhibitors

drugs, ind, administration

A
  • Entacapone
    • Block L-DOPA metabolism in periphery (COMT-inhib)
    • IND:
      • parkinsons disease (prolongs L-dopa actions)
    • oral
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11
Q

COMT-I SE

A
  • entacapone, tolcapone
  • related to increased L-DOPA levels
  • sleep disorders
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12
Q

Amantidine MOA , admin, eliminatio

A
  • anti-viral medication
  • enhances dopaminergic neurotransmission by:
    • increasing synthesis/release
    • or decreases reuptake of dopamine.
  • Muscurinic-block
  • NMDA receptor antagonists with neuroprotective properties. (like memantine)

oral

renal elimination

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13
Q

Amantidine clinical use

A
  • Parkinsons disease (adjunct to levo-dopa/carbidopa)
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14
Q

Amantidine SE

A
  • livedo reticularis ( dermatological)
  • psychosis
  • GI disturbances
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15
Q

Procyclidine MOA,

A
  • Anti-muscurinic (Ach blocking agent)
    • decreases excitatory acitivity of cholinergic neurons
    • improves tremor and rigidity
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16
Q

Procyclidine, adminis, clinical use

A
  • oral
  1. parkinsons disease (not recommended as monotherapy in early disease)
  2. drug induced extra-pyramidal symptoms
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17
Q

Procyclidine SE

A
  • atropine like effects
    1. dry mouth
    2. urinary retension
    3. constiptaion
    4. hyperthermia
    5. sinus tachy
    6. mydriasis
    7. blurred vision
    8. toxicity: cardiotoxic, convulsions, coma
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18
Q

Procyclidine CI

A
  • glaucoma
  • prostatic hyperplasia
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19
Q

Alzheimer drugs

A

Rivastigmine- AchE inhib.
Memantine- NMDA-R blocker
אתה ממתין שסבתא תיזכר כי יש לה אלצהיימר

Piracetam- nootropic. Helps with cognitive functions
זו תרופה שהיא פיראטית

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20
Q

Rivastigmine

MOA, IND, Administration, SE

A
  • Ach-Esterase inhibitor (centrally acting)
  • oral
  • IND:
    • alzhiemers (1st line);
      (modest reduction in rate of congnitive function loss)
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21
Q

AchE inhibitor rivastigmine SE

A

SE:

​

  • bradycardia
  • diarhhea
  • nausea, vomit
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22
Q

Memantine MOA, IND, Administration

A
  • glutamate NMDA-R blocker
  • oral
  • alzhiemers disease
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23
Q

memantine se

A

SE:

  • Confusion
  • Agitation
  • Restlessness
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24
Q

Nootropic drug

A
  • Piracetam
    • interferes with neurotransmitter realease by binding to synaptic vesicle protein (SV2A) ( protein involved in vesicle docking, fusion
  • therapeutic potential as congitive enhancer in treatment of
    • schizophrenia
    • depression
    • ADHD
    • PARKINSONS
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25
Q

Drugs for GI spasm and uterus

A
  • Butyl-scopolamine
  • Solifenacin, Oxybutinin
  • Papaverine
  • Drotaverine
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26
Q

Butyl-scopolamine MOA, IND

A
  • M-blocker non selective
  • quaternary amine
  • IND :
    • smooth m spasm
    • abdominal, menstural cramps
    • spasmodic activity in GI , GU tracts
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27
Q

Solifenacin, oxybutinin MOA, administration, doa

A
  • competitive antagonist (inverse agonist at all M-r but modest selectivity for M3
  • Oxybutynin: oral, transdermal,
  • solifencacin : Oral
  • Duration: 12–24 h
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28
Q

SOLIFENACIN, OXYBUTININ indicatio

A

ind:

  • hyperactive bladder syndrome
  • urinary urgency, incontinence
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29
Q

Papaverine and Drotaverine moa

A

PAPA help me! Drota! like when you curse

  • CCB
  • PDE-Inhibitor ( non selective)
  • opioid alkaloid derivative
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30
Q

papaverine, drotaverin Administration, IND

A
  • oral, parenteral

IND:

* GI, GU spasms
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31
Q

Agents relaxing pregnant uterus

A
  • Atosiban-
    • Oxytocin antag. לעכב לידה Ato for Atopic
    • I.V infusion
    • IND: Tocolysis for preterm labor
    • effective from gestational week 24
  • Terbutaline-
    • SABA. (Beta-2 selective agonist)
    • IND:
      • Relaxation of pregnany uterus
      • Prompt onset for acute bronchospasm
    • Aerosol inhalation, parenteral, oral
  • Mg-sulfate
    • i.v
    • IND:
      • tocolytic agent
      • seizure prevention in preeclampsia/eclampsia
      • protective role on fetal brain
      • Ethanol
    • ​tocolytic
    • I.V
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32
Q

Atosiban- MOA, ADMINISTRATION

A
  • Oxytocin antag. לעכב לידה Ato for Atopic
  • I.V infusion
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33
Q

atosiban ind , se

when is it effective

A
  • IND: Tocolysis for preterm labor
  • se:
    • Concern about rates of infant death
    • not FDA approved

effective from gestational week 24

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34
Q

Terbutaline-

MOA, admin route

A

SABA. (Beta-2 selective agonist)

Aerosol inhalation, parenteral, oral

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35
Q

terbutaline ind

A

IND:

  • Relaxation of pregnany uterus
  • Prompt onset for acute bronchospasm
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36
Q

Mg-sulfate

Administration, IND

A
  • i.v
  • IND:
    • tocolytic agent
    • seizure prevention in preeclampsia/eclampsia
    • protective role on fetal brain
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37
Q

Mg-sulfate SE

A

SE:

  • maternal :
    • lethargy,
    • headache,
    • weakness,
    • pulmonary edema,
    • cardiac arrest
  • neonatal
    • hypotension,
    • respiratory depression
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38
Q

location of H1-receptor and prototypic antagonist

A
  • H1:
    • Brain, Endothelium, Smooth muscles, (BES)
    • Gq coupled (IP3, DAG) IGE-mediated response :
    • Prototypic antagonist: Diphenhydramine, loratidine
    • .

QSII

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39
Q

location of H2-r and antagonist

A

H2:

  • Brain, Heart, Mast cell, Stomach (BHMS)
  • Gs coupled (cAMP)
    • mediates gastric acid secretion by parietal cells
      • cardiac stimulant effect
      • negative Fb reduces histamine release from mast cells:

Cimetidine

QSII

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40
Q

H3- receptor location , mechanism, antagonist

A

H3:

  • ​CNS, Nerve endings (CN) -
  • Gi (decrease cAMP) mediates
    • presynaptic modulation of histaminergic neurotransmission in CNS,
    • increases apetite
    • in periphery its a presynaptic heteroR with modulatory effects on release of other transmitters ( adrenergic n transmission) :

Clobenpropit (investigational)

  • No agonist or antagonist of H3 and H4 receptors are available for clinical use

QSII

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41
Q

H4-r location, mechanism, antagonist

A

H4:

  • CD4-T cells,
  • Leukocytes (esp eosinophils),
  • mast cells-

Gi involved in chemotactic response :

Thioperamide

  • No agonist or antagonist of H3 and H4 receptors are available for clinical use

QSII

42
Q

Enhanced cervical dilation

A

Drotaverine

43
Q

Tocolytic drug meaning

A

Designed to inhibit contractions of myometrial smooth muscle cells

delay your delivery for a short time (up to 48 hours) if you begin labor too early in your pregnancy.

44
Q

Agents contracting uterus

A

OME is a women

  • Oxytocin:
    • ​oxytocin-r agonist
    • I.V , intranasal
    • ind:
      • induction and augmentation of labor
      • control of postpartum uterine hemmorage (high dose)
      • induction of lactation (intranasal)
    • SE:
      • fetal distress, placental abruption, uterine rupture
  • Misoprostol-
    • PGE1 analog. סיום הריון 60 יום
    • oral
    • causes abortion in combo with mifepristone (progesterone antagonist)
    • effective up to 60 days into pregnancy
  • Ergotamine-
    • induces vasoconstriction and uterine contraction
    • ergot alkaloid derivative
    • parenteral
    • ind:
      • control of postpartum bleeding
    • (DONT give before delivery of placenta)

Misoprostol+Mifepristone

45
Q

Oxytocin MOA , administration

A

​oxytocin-r agonist

I.V , intranasal

46
Q

oxytocin ind

A

ind:

  • induction and augmentation of labor
  • control of postpartum uterine hemmorage (high dose)
  • induction of lactation (intranasal)
47
Q

oxytocin SE

A

SE:

  • fetal distress,
  • placental abruption,
  • uterine rupture
48
Q

Misoprostol-

MOA, ADMINS

A

PGE1 analog. סיום הריון 60 יום

oral

49
Q

Misprostol ind, till when is it effective

A
  • causes abortion in combo with mifepristone (progesterone antagonist)

effective up to 60 days into pregnancy

50
Q

Ergotamine-

MOA, doa

A
  • Partial agonist at
    • 5-HT
    • Alpha r
      • esp in blood vessels, uterus
  • ergot alkaloid
  • 10-12hr
51
Q

ergotamine effect on vessel and uterus

A

induces vasoconstriction and uterine contraction

52
Q

ergotamine ind, administration

CI

A

parenteral

ind:

  • control of postpartum bleeding
  • migraine
  • cluster headache

(DONT give before delivery of placenta)

53
Q

ergotamine SE

A
  • Nausea, vomiting, diarrhea,
  • severe vasospasm
54
Q

drugs acting on Male reproductive

A

Tamsulosin-

  • competitive antagonist at alpha-1 . ( Alpha1-selective blockers )
  • BPH : reduce urinary hesitancy and prevent urinary retention in men with benign prostatic hyperplasia.
    • relaxes muscle of prostate and neck of bladder
  • SE: orthostatic hypotensive response to the first dose, little reflex tachy

Sildenafil- PDE-5 inhib.

  • erectile dys
  • pulmonary hypertension
  • SE:
    • priapism (prolonged erection)
    • severe hypotension in combo with nitrates
    • blue-tinted vision (via inhibiting PDE-6 in retina)
55
Q

Antiemetics

A

Piiii DOM DAD blahhhs it make me vomit

  • *Dimehydrinat**- H1 blocker
  • *Ondansteron**- 5HT3 blocker
  • *Palonosteron “**5HT3 blocker
  • *Metoclopramide**- D2 blocker
  • *Droperidol** D2 blocker
  • *Aprepitant**- NK1 antagonist
  • *Dronabinol**- CB1 cannabinoid agonist. When you smoke weed you feel like yor dron and you want to eat bino shawarma
56
Q

Serotonin receptors location and antagonist

A
  • 5-HT 1D/1B : Brain (Gi) —–
  • 5-HT2 : Brain, Smooth m, Platelets (Gq) : ketanserin
  • 5-HT3: Area postrema(CNS), Sensory nerves, Enteric nerves (ligand gated Na/K ch) : Odansetron
  • 5-HT4 : presynaptic nerve terminals in the ENS (Gs) : Tegaserod (partial agonist)

iq- ligand gated - s

57
Q

5-HT1D/1B receptor location, action

A
  • brain
  • Gi , decreases cAMP
  • IQ - ligand gated Na/K - I (all serotonin receptors mnemonic )
58
Q

5-HT2

location,

receptor mechanism,

antagonist

A
  • Smooth muscle
  • platelets
  • brain. (BPS)
  • Gq; ↑ IP3, DAG

Ketanserin

59
Q

5-HT3

location

action

antagonist

A
  • Area postrema (CNS),
  • sensory nerves
  • enteric nerves

Ligand-gated Na+/K+ channel

ondansetron

60
Q

5-HT4

location

action

antagonist

A
  • Presynaptic nerve terminals in the enteric nervous system

Gs; ↑ cAMP

Tegaserod

61
Q

dimenhydrinate

MOA, DOA

A
  • H1 blockers, first generation (Diphenhydramine, dimenhydrinate)
  • MOA:
    • Competitive block of peripheral & CNS H1 receptors
      • α-block + M-receptor block.
    • Anti-motion sickness effect
  • DOA: 6-8 hrs
62
Q

dimenhydrinate IND, admin

A

IND:

  • motion sickness
  • Anti-emetic
  • used orally as OTC sleep aid;

adm: Oral, parenteral

63
Q

dimenhydrinate SE

A

SE:

  • Sedation
  • autonomic block
  • Rare CNS excitation
64
Q

Ondansteron- Palonosteron

MOA

A
  • 5-HT3 Blocker : Ondansetron, Palonosteron
  • blocks chemoreceptor trigger zone + enteric nervous system 5-HT3 receptors
65
Q

ondansteron, Palonosteron

IND

,administration

A

IND: Anti-emetic

  • Chemotherapy, radiation induced vomiting
  • postoperative vomiting

Oral, IV

66
Q

ondansteron, Palonosteron

DOA, SE

A
  • Duration: 3–6 h

SE:

  • QT prolongation,
  • possible arrhythmias,
  • May slow colonic transit
67
Q

Metoclopramide-
MOA

A
  • Prokinetic agents
  • D2 receptor blocker ;
    • increases gastric emptying and intestinal motility (area postrema is also of value in preventing emesis )
68
Q

Prokinetic agents :

A
  • Metoclopramide, (D2 receptor blocker)
  • domeperidone, ( like metroclopramide but less CNS effct
  • cholinomimmetics
    • (neostigmine):
      • for colonic pseudo-obstruction in hospitalized patients
  • Macrolides:
    • erythrornycin useful in diabetic gastroparesis but tolerance develops
69
Q

Metoclopramid, IND , administra

A

IND: Anti-emetic

  • Gastric paresis (eg, in diabetes)
  • antiemetic (surgical anasthesia, chemotheraperutic drugs)

Oral and parenteral formulations

70
Q

metoclopramid se

A

SE:

  • if chronic use can cause
    • Parkinsonian symptoms due to block of CNS D2 receptors
    • other extrapyramidal effects
    • Hyperprolactinemia.
71
Q

Droperidol

MOA

A
  • potent D2 blocker
    • alpha-1 blocker
72
Q

droperidol

ind, se

A

IND:

  1. anti-pscyhotic
  2. anti-emesis (CHEMO, RADIO, post operative)

SE:

prolong QT

73
Q

Aprepitant-
MOA

A
  • neurokinin 1 (NK1) blocker
  • moa: Tachykinin NK1 receptor blocker
74
Q

aprepitant ind

A
  • IND:
    • ANTI-emetic for chemotherapy-induced nausea and vomiting
75
Q

aprepitant se

A

SE:

  • fatigue,
  • dizziness,
  • diarrhea,
  • P450 interactions

se: Asthenia, hiccups

76
Q

APREPITANT

administration, doa

A

oral

Half-life: 9–13 h

77
Q

Dronabinol

MOA

ind

se

A
  • CB1 cannabinoid agonist
  • Anti-emetic
  • for use in chemotherapy-induced nausea and vomiting,
  • SE: associated with CNS marijuana effects
78
Q

Drugs used for IBS

A
  • 5HT-3 blocker : Alosetron
    • Severe diarrhea-predominant IBS in women
    • oral
    • SE: due to se restricted use!
      • Rare but serious constipation
      • ischemic colitis
      • bowel infarction
  • Anticholinergics: nonselective action on GI activity; associated with typical antimuscarinic toxicity
    • dicyclomine and hyoscyamine are used as antispasmodics to relieve abdominal pain but efficacy not convincing
  • Chloride channel activator: lubiprostone = laxative (activate type 2 Cl- ch in small intestine)
    • in constipation-predominant IBS in women
79
Q

Laxative

A
  • Irritants and stimulants :
    • Sennoside the colon is So Blocked!
    • Bisacodyl-
  • Bulk-forming laxative:
    • Plant fiber- lubrication
  • osmotic laxatives
    • Mg-sulfate/oxide/citrate
    • Lactulose
  • lubricant laxative:
    • Paraffin oil
80
Q

Irritants and stimulants (laxative)

A

the colon is So Blocked!

  • Sennoside.
    • a natural complex of anthraquinone glycosides
    • its degradation product acts as irritant on colonic wall > induces fluid secretion and colonic motility
    • oral, rectal
  • Bisacodyl
    • potent stimulant of colon, acts on nerves in colonic mucosa
81
Q

bisacodyl SE

A

SE:

  • abdominal cramps
  • atonic colon (prolonged use)
  • damage to enteric protective coating
82
Q

Bulk-forming laxative:

A
  • Plant fiber- (methylcellulose) :
    • indigestable parts of fruits, vegetable
    • forms gel in colon> water retension > intestinal distension > increased peristalsis
    • increase volume, stimulate evacuation
83
Q

osmotic laxatives

A
  • Mg-sulfate/oxide/citrate
    • osmotic agents (non-absorbable salt) increase water content in stool.
    • oral
    • IND:
      • Simple constipation
      • bowel prep for endoscopy (especially PEG solutions)
      • SE: Mg may be absorbed and cause toxicity in renal impairment
  • Lactulose
    • cannot be hydrolysed by intestinal enzymes
    • oral, degraded by colonic bacteria into lactic , formic, acetic acid
    • also used in hepatic encephalopathy (decreases ammonia)
84
Q

lubricant laxative:

A

Paraffin oil

  • Acts by facilitating passage of hard stool (lubricant)
  • taken orally, in upright position to avoid aspiration and lipid pneumonia
85
Q

Antidiarrheal

A

Eating DAL is good for you gut

  • Diphenoxylate, Loperamide- (oral)
    • opioid derivatives, P450 metabolism
    • activate u-opioid receptors in ENS (inhibits Ach release)
  • Activated charcoal
    • ​attract and expel ingested toxins from GI tract
    • oral
    • IND: non specific, non infecious diarrhea
86
Q

Diphenoxylate, Loperamide

MOA, indication, administration

A
  • (oral)
  • opioid derivatives, P450 metabolism
  • MOA- activate u-opioid receptors in ENS (inhibits Ach release)
    • slows motility
    • negligible CNS effect ( diphenoxylate high doses can cause CNS opioid effects and toxicity)
  • IND: non-specific, non-infecious diarrhea

se:Mild cramping but little/no CNS effect

87
Q

Liver and biliary drugs

A
  • *N-acetylcysteine**- Acetaminophen toxicity
  • *Sillimarine**- for alcohol liver injury

ursodeoxycholoc acid

This silly marine drunk too much!!

88
Q

N-acetylcysteine MOA , characteristics, clinical use , se

A
  • provides SH groups
  • oral, I.V , inhaled
  • T1/2 =5-6 hrs
  • P450 metabolism
  • IND:
    • acetaminophen toxicity (within 8-10 hrs of overdose)
    • mucolytic agent (used in COPD , CF)
  • SE:
    • nausea, vomit,
    • anaphylaxis-like allergic rxn
89
Q

Sillimarine MOA, characteristic, clinical use, SE

A
  • derived from fruit and seeds of silybum marianum
  • support liver function
  • oral
  • IND:
    • Protects against liver injury caused by
      • alcohol
      • acetaminophen
      • amanita mushroom
    • antidote to amanita phalloides mushroom poisoning
90
Q

ursodeoxycholoc acid (Ursodiol)

moa, characterictics

A
  • Reduces cholesterol secretion into bile > dissolve cholesterol gallstones
  • potential anti-inflammatory effect in GI
  • oral
91
Q

ursodeoxycholoc acid (Ursodiol)

Clinical use, SE

A
  • IND:
    • Gallstones in patients refusing or not eligible for surgery
    • primary biliary cirhosis (PBC)

SE: little/no toxicity , diarhhea

92
Q

drugs used in peptic ulcer disease

A
  • Antacids-
    • MgO , Aluminum-hydroxide
  • H2-R antag.-
    • Famotidine. peptic ulcer is in the FAMily TIDINE is for allery suffix
  • PPI-
    • (es) Omeprazol and Pantoprazol (Panting!)
  • Mucosal protection-
    • Sucralfate. Sugar fate is into the stomach. protective gel like
93
Q

Antacids-

drugs, administration, clinical use, SE

A
  • MgO , Aluminum-hydroxide
    • ​oral
    • poorly absorbed from bowel
  • OTC for symptomatic relief of heartburn
  • Not as useful as PPI and H2-blocker in peptic diseases

SE of MgO: diarhhea

SE: Al2(OH)3 : constipation

94
Q

H2-R antag.-

drugs, administration routes, DOA

A
  • Famotidine, cimetidine, nizatidine, ranitidine peptic ulcer is in the FAMily TIDINE is for allery suffix
    • oral, parenteral
    • DOA: 12-24 hrs
    • CYP450 metabolism, inhibitor of cyp450 enzymes
      • reduce nocturnal acid but less effective than PPIs against stimulated secretion
      • very safe, available over the counter (OTC).
      • Cimetidine, but not other H2 blockers, is a weak antiandrogenic agent and a potent P450 enzyme inhibiton
95
Q

H2-R blocker drug and SE

A
  • famotidine, cimetidine, nizatidine, ranitidine
  • SE:
    • GI distress
    • antiandronergic effects : gynecomastia, decreased libido ( cimetidine)
    • confusion, agitation (elderly)
    • milder drug interactions
96
Q

famotidine indication

A

reduce nocturnal acid but less effective than PPIs against stimulated secretion

very safe, available over the counter (OTC).

Cimetidine, but not other H2 blockers, is a weak antiandrogenic agent and a potent P450 enzyme inhibiton

ind:

  • GERD
  • PUD
  • H.pylori ass ulcers
  • NSAIDs induced ulcers
  • prophylaxis against stress-related mucosal injury
  • Zollinger elson syndrome
97
Q

PPI-

MOA, DOA , administration route

full supressing effect achieved in how many days?

A
  • (es) Omeprazol and Pantoprazol (Panting!)
    • Irreversible blockade of H+/K+ ATPase in active gastric parietal cells
    • oral (on empty stomach) , I.V
    • Half-lives much shorter than duration of action (T1/2= 1-2 hrs)
    • full supressing effect achieved in 3-4 days
98
Q

PPI- indication

A

IND:

  • Peptic ulcer,
  • GERD,
  • erosive gastritis
99
Q

PPI SE

A

SE:

Low toxicity:

  • diarrhea,
  • abdominal pain,
  • headache.
  • hypergastrinemia (Chronic treatment )
  • decrease oral bioavalability of VITB12 and drugs which require acidic environment for GI absorption (digoxin, ketoconazole)
  • small increase in the risk of respiratory and enteric infections
  • reduction of stomach acid may reduce absorption of some drugs and increase that of others
    • eg: omeprazole inhibits CYP450 ; effects
      • warfarin
      • phenytoin
      • diazepam
100
Q

Mucosal protective agent in PUD

administration, MOA, SE

A
  • Sucralfate. Sugar fate is into the stomach. protective gel like
    • oral, 4x daily
    • prodrug: requires acidic pH ( antaacid, ppi, H2blocker interefe)
    • MOA: polymerizes at site of tissue damage and protects against further damage
    • very insoluble with no systemic effects
    • SE: constipation
101
Q

Sucralfate indication

A

IND:

  • improves healing after mucosal damage
  • prevent re-occurance
102
Q

Drugs acting on smooth muscle - contraction

A

*controlled by ANS, hormones.

  • through Ca +2 DIRECT
  • cAMP>>MLCK (P/dephosphorylation)

Contraction:

  • Neurotransmitter:
    • ​Ach (M) : Betanechol (urinary retension), pilocarpine (glaucoma, contract ciliary m> increase aquous humor> decrease IOP
    • E/NE = endogenous mediator , act by alpha-1
  • Autacoids= endogenous molecules which don’t fall into traditional autonomic groups. They DONT act on cholinoR nor adrenoR but have powerful pharmacologic effect on smooth m and other tissue. They are produced at site of action and act there as local mediator. Short acting compounds, with broad spectrum of biological activity; acts on smooth m
    • Histamine (biogenic amine)
    • Serotonin (5-hydroxytryptamine) - biogenic amine
    • Eicosanoids= arachidonic acid derivative (PG, LT)
      • ​PGE2 (natural dinoprost) - used in gynecology + contraction for labour
      • PGF2 (carboprost)
      • TXA2
      • LTD4, LTE4 : important in bronchoconstriction
  • Angiotensin , VIP, Kinins
  • Polypeptides :
    • ​Oxytocin
    • Angiotensin II
    • Endothelin (ETR1 |—- Bosertan (ETR1 BLOCKER) –> pulmonary hypertension
  • ATP-derivatives

Pharmacology FINAL (2nd sem) (37 decks)

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