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5. Pharmacology AC > Topic list A drugs > Flashcards

Topic list A drugs Flashcards

1
Q

Drugs acting on GI and UroG SM by inducing smooth muscle relaxation (5)

A
  1. Papaverine
  2. Drotaverine
  3. Butyl-scopalamine
  4. Solifenacin
  5. Oxybutynin
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2
Q

Tocolytic drugs - that relax the pregnant uterus (4)

A
  1. Atosiban
  2. Terbutaline
  3. Mg2+
  4. Ethanol
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3
Q

Drugs that contract the pregnant uterus (3)

A
  1. Oxytocin
  2. Ergotamine
  3. Misoprostol
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4
Q

Agents acting on the male reproductive system

A

Tamsulosin

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5
Q

1st generation H1 receptor antagonists

A
  • Diphenhydramine
  • Dimetindene
  • Promethazine
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6
Q

2nd generation H1 receptor antagonists

A
  • Levocetirizine
  • Desloratadine
  • Fexofenadine
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7
Q

Papaverine, drotaverine
- MOA
- Indication
- Side effects
- ROA

A
  • Calcium channel blockers and non selective phosphodiesterase inhibitor
  • GI and urogenital spasm
  • Hypotension, arrythmias, hepatotoxicity
  • Oral and parenteral
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8
Q

Butyl-scopalamine
- MOA
- Effect
- Indications

A
  • Non-selective muscarinic antagonist
  • SM relaxation (GI!)
  • Pain and discomfort caused by abdominal cramps or urinary tract spasms
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9
Q

Difference between butyl-scopalamine and scopalamine

A

Butyl-scopalamine has no CNS effects

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10
Q

Solifenacin, oxybutinin
- MOA
- Effects
- ROA
- Extra

A
  • Selective muscarinic antagonist : M3 (Gq receptor -> contraction)
  • Relax the muscles in the wall of the bladder and decrease detrusor muscle spasms
  • Oral or transdermal patch
  • Short acting
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11
Q

Atosiban
- MOA
- Indication
- Side effects
- ROA

A
  • oxytocin receptor antagonist (Gq receptor)
  • Prevents premature labor
  • Increased rates of infant death
  • IV
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12
Q

Terbutaline
- MOA
- Effect
- Indication
- Side effect
- ROA

A
  • Short acting B2 agonist (Gs coupled)
  • Uterus relaxation (and bronchodilation)
  • To prevent premature labor (from 16th week)
  • Arrythmias
  • Aerosol inhalation, oral, parenteral
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13
Q

Mg2+
- MOA
- Indication
- Side effects
- ROA

A
  • Calcium channel blocker
  • To relax the uterus
  • Maternal SE : flushing, lethargy, pulmonary edema, cardiac arrest
  • Neonatal SE : hypotension, respiratory depression
  • ROA : IV
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14
Q

MOA of oxytocin

A

Oxytocin receptor is GQ coupled

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15
Q

Oxytocin
- Effect
- Indication
- SE
- ROA

A
  • Contraction of uterus and of the myoepithelial cells of the breast
  • Induction of labor, decrease of postpartum hemorrhage, induction of lactation
  • Fetal distress, placental abruption, uterine rupture, hypervolemia (4)
  • IV, intranasal
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16
Q

Ergotamine
- MOA
- Effect
- Indication
- Contraindication
- Side effects
- ROA

A
  • alpha 1 (Gq coupled) and 5HT-R agonist
  • Induce vasoconstriction and uterine contraction
  • To prevent postpartum uterine hemorrhage
  • HT, pregnancy
  • Increased BP, angina
  • Parenteral
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17
Q

Misoprostol
- MOA
- Effect
- Indication
- Side effects
- ROA

A
  • Prostaglandin E1 analog (Gq)
  • Uterus contraction, gastric mucus secretion
  • For abortion or to induce labor + postpartum hemorrhage
  • Bleeding
  • Oral
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18
Q

Tamsulosin
- MOA
- Effect
- Indication
- ROA

A
  • Alpha1 selective antagonist (Gq coupled)
  • Relax the muscles of the prostate + bladder neck
  • BPH, hypertension
  • Oral
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19
Q

Diphenhydramine and dimetindene
- MOA
- Effects
- Indication

A
  • H1 (1st generation), Alpha1-AR, muscarinic, and serotonergic antagonist
  • Decreases vascular permeability and nasal and bronchial mucus secretion + causes bronchorelaxation
  • For IGE mediated allergies, asthma bronchiale and anaphylaxis mainly. Nausea, vomiting, dizziness, anorexia sometimes.
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20
Q

Side effects of diphenhydramine and dimetindene

A
  • Sedation, cognitive impairment
  • Antimuscarinic : dry mouth, blurred vision, glaucoma exarcerbation
  • Antiadrenergic : hypotension
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21
Q

Indication of 2nd generation H1 receptor antagonists

A

IGE mediated allergies (hay fever, urticaria…)

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22
Q

Side effects of 2nd generation H1R antagonists

A

Sedation and K+ channel inhibition at high doses

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23
Q

What is the action of fampridin (4-aminopyridin)?

A

It binds to M2 and blocks K+ channels when in the open position, which causes the depolarization to last longer and helps propagation in demyelinised axons

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24
Q

What is the effect of the botulinum toxin on cholinergic transmission?

A

It inhibits the terminal calcium channel, which stops the signal for vesicular release

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25
Q

Levodopa
- MOA
- Effect
- Indication
- Side effects (5)

A
  • Metabolic precursor of dopamine
  • Increases the activity of DOPA-decarboxylase
  • Parkinson’s disease
  • Dyskenia, hypotension, arrythmias, nausea, depression
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26
Q

What is the effect of carbidopa?

A

It inhibits DOPA-decarboxylase and prevents synthesis of dopamine peripherally

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27
Q

What is the effect of metyrosine

A

Inhibits synthesis of DOPA from tyrosine

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28
Q

Cholinomimetics that are direct muscarinic and/or nicotonic agonists

A
  • carbachol
  • pilocarpine
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29
Q

Cholinomimetics that are indirect agonists

A
  • Neostigmine
  • pyridostigmine
  • rivastigmine
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30
Q

Carbachol
- MOA
- Effect

A
  • Muscarinic and nicotinic agonist
  • Miosis via ciliary muscle contraction (M3) and decreased intraocular pressure
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31
Q

What is the MOA of pilocarpine?

A

Direct muscarinic agonist

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32
Q

What is the effect of pilocarpine?

A

Increases salivation and sweat production

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33
Q

What are the indications of neostigmine and pyridostigmine?

A

Reverse the effects of relaxants and for treatment of myasthenia gravis

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34
Q

What is special about neostigmine and pyridostigmine?

A

They are quaternary amine and do not cross the BBB

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35
Q

Rivastigmine
- MOA
- Indication
- Side effects

A
  • Cholinesterase inhibitor
  • For the treatment of mild dementia of alzheimer type
  • Nausea, vomiting, bradycardia
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36
Q

8 examples of muscarinic antagonists (receptor blocking)

A
  • Atropine
  • Butyl-scopalamine
  • Procyclidine
  • Cyclopentolate
  • Ipratropium
  • Tiotropium
  • Solifenacin
  • Oxybutinin

at pro cyclist tournaments, i solely binge oxy

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37
Q

Which muscarinic receptor blocking drugs are selective?

A

Tiotropium, solifenacin and oxybutinin are selective M3 antagonists

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38
Q

How is butyl-scopalamine different from scopalamine?

A

It cannot enter the CNS

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39
Q

Procyclidine
- MOA
- Indications

A
  • Muscarinic receptor antagonist
  • Parkinson’s disease (increase in Ach due to decrease in dopamine)
  • Extrapyramidal disorders caused by drugs
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40
Q

Can procyclidine enter the CNS?

A

Yes, it has a tertiary amine

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41
Q

What is the indication of cyclopentolate?

A

It is used to dilate the pupils in ophtalmologic examinations

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42
Q

ipratropium and triotropium
MOA
Effect
ROA

A
  • Muscarinic antagonist
  • Bronchodilation
  • Inhaled from a spray
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43
Q

MOA of epinephrine (small and large dose)

A
  • Small dose : B stimulation predominates
  • Big dose : A1 stimulation predominates
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44
Q

Epinephrine doses

A
  • Anaphylaxia : 0.15-0.5mg or 0.05-0.1mg in IV
  • Resuscitation : 1mg IV
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45
Q

Norepinephrine
- MOA
- Effect
- Indications

A
  • a1, a2 and b1 agonist
  • Vasoconstriction
  • Acute hypotension in shock + cardiac arrest / complete heart block
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46
Q

MOA of dopamine (small, medium and large dose)

A
  • small : D1 - vasodilation, increase in GFR
  • medium : D1, b1 - positive inotropic & chronotropic effect
  • large dose : a1 effect - vasoconstriction
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47
Q

Indications of dopamine (3)

A
  • Shock
  • Renal insufficiency
  • Heart failure
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48
Q

Dobutamine
- MOA
- Effect

A
  • b1 agonist
  • Cardiac Output and Stroke Volume increase
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49
Q

Isoprenaline
- MOA
- Effect
- Contraindications

A
  • Non selective b-agonist (it’s one of the catecholamines)
  • Positive inotropic and chronotropic effect via b1+ bronchodilation via b2
  • Underlying coronary disease
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50
Q

Ephedrine
MOA
Indications (3)

A
  • Indirect sympathomimetic + weak b2 agonist
  • Nasal decongestant + Treatment of anesthesia related hypotension + Appetite suppressant
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51
Q

Phenylephrine
- MOA
- Indications (3)

A
  • a1 agonist
  • Hypotension, nasal decongestion, mydriasis for ophtalmologic examination
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52
Q

MOA of oxymetazoline

A
  • Local a1 agonist
  • Systemic a2 agonist
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53
Q

Clonidine
- MOA
- Effects
Indications (3)

A
  • a2 agonist (Gi coupled - inhibitory)
  • Presynaptic a2R leads to decrease in release of NE and thus a decrease in BP
  • Hypertension, Tourette’s, ADHD
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54
Q

MOA of Rilmenidine

A

A2 agonist

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55
Q

Methyldopa
- MOA
- Extra

A
  • A2 agonist
  • It can be used even during pregnancy because it can’t activate other adrenergic receptors
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56
Q

3 a1-selective antagonist drugs

A
  • Prazosin
  • Doxazosin
  • Tamsulosin
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57
Q

Effect of prazosin, doxazosin, tamsulosin

A

Relax muscle of prostate + bladder neck

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58
Q

MOA of urapidil

A
  • a1 selective antagonist
  • a2 agonist
  • b antagonist
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59
Q

Carvedilol
- MOA
- Indications

A
  • a1 selective antagonist and b antagonist
  • Hypertension, CHF, chronic stable angina

(It decreases HT through alpha and reduces tachycardia, heart problems through beta)

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60
Q

Phentolamine
- MOA
- Effect
- Indication

A
  • Non selective a-antagonist
  • Vasodilation
  • Treatment of pheochromocytoma & acute hypertension due to a-agonist overdose
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61
Q

4 non-selective beta antagonists

A
  • Propanolol
  • Pindolol
  • Timolol
  • Sotalol
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62
Q

4 beta1-selective antagonists

A
  • Bisoprolol
  • Metoprolol
  • Esmolol
  • Nebivolol
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63
Q

Indications for b1-selective antagonists

A
  • Hypertension
  • Chronic stable angina
  • CHF
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64
Q

Dosage of metoprolol

A

2x25-100mg

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65
Q

Which b-selective antagonists cross the BBB?

A

Bisoprolol and nebivolol because they are lipophilic

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66
Q

Which local anesthetics are amides?

A
  • Lidocaine
  • Articaine
  • Bupivacaine
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67
Q

Which local anesthetics are esters?

A
  • Cocaine
  • Benzocaine
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68
Q

What is the MOA of local anesthetics?

A

Na+ channel blockers

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69
Q

Lidocaine
- Indications (3)
- Duration of action

A
  • Local surgical procedures, post operative analgesia and ventricular arrhythmia
  • 1-2 hours, 2-4 hours if combined with epinephrine
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70
Q

Cocaine
MOA
Effect

A
  • binds and inactivates sodium channels, which inhibits excitation
  • blocks NE reuptake into nerve terminals because of its vasoconstrictive properties : intrinsic sympathomimetic effect
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71
Q

Effect of benzocaine

A

Reversibly stabilizes the neuronal membrane - decreases its permeability to Na ions : anesthetic

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72
Q

What type of receptors are the opioid receptors?

A

They are all Gi coupled

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73
Q

What is the MOA of morphine?

A

Strong opioid receptor agonist

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74
Q

Cite 6 main effects of morphine

A
  1. Analgesia
  2. Respiratory depression
  3. Decreased BP + bradycardia
  4. Nausea, vomiting
  5. Bronchoconstriction
  6. Urinary retention & constipation
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75
Q

Dosage of morphine (per os / sc / iv)

A
  • Per os : morphine sulfate - 2x 30-100mg
  • Sc : morphine hydrochloride - 10-20mg
  • IV : morphine hydrochloride - 1mg (repeated up to 10mg)
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76
Q

Codeine
- MOA
- Effects

A
  • Weak agonist of MOR - mu opioid receptor
  • Antitussive and weak analgesic effect
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77
Q

Aspirin / acetylsalicilic acid
- MOA
- Effect
- Side effects (4)

A
  • Irreversible COX inhibitor
  • Inhibition of COX enzyme in platelets decreases thromboxane A2, which decreases platelet aggregation
  • Bleeding, peptic ulcers, hypersensitivity reaction, respiratory alkalosis -> respiratory acidosis
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78
Q

Dose-dependant effects of acetylsalicilic acid

A
  • 50-200mg/day : inhibition of platelet aggregation
  • 500mg/day : analgesic and antipyretic
  • 4-5g/day : anti-inflammatory
79
Q

What drug is used for management of acute gout attacks?

A

Colchicine

80
Q

Colchicine
- MOA
- Side effects (3)

A
  • Microtubule assembly inhibitor -> inhibits mitosis
  • Hepatotoxic, Neurotoxic, Nephrotoxic
81
Q

Drugs used for management of chronic gout

A
  1. Allopurinol
  2. Rasburicase
82
Q

MOA of allopurinol

A

Uric acid synthesis inhibitor

83
Q

MOA of rasburicase

A

Recombinant type of urate oxidase : decreases serum uric acid by transforming uric acid into allantoin

84
Q

List of centrally acting muscle relaxants (6) aka spasmolytics

A
  1. Diazepam
  2. Baclofen
  3. Tizanidine
  4. Tolperisone
  5. Dantrolene
  6. Botulinum toxin
    (2B2D2T acronym)
85
Q

Diazepam
- MOA
- Effect
- Indications
- Dosage

A
  • GABA(a) receptor agonist (increases GABA(a) effect)
  • Cl influx -> hyperpolarization -> muscle relaxant effect
  • Chronic and acute spasm
  • Dose : 5-10mg, but for status epilepticus : iv 30mg
86
Q

Baclofen
- MOA
- Effect

A
  • GABA(b) receptor agonist
  • Gi coupled receptor -> K+ efflux -> hyperpolarization -> long lasting muscle relaxant
87
Q

Tizanidine
- MOA
- Effect

A
  • alpha 2 agonist (Gi coupled)
  • causes pre-synaptic stimulation of alpha 2 R -> inhibition of glutamate release -> muscle relaxation
88
Q

MOA and effect of tolperisone

A
  • MOA is unknown
  • Causes reduction of the muscle reflex
89
Q

Dantrolene
- MOA
- Effect
- Indications

A
  • Ryanodine receptor antagonist
  • Inhibits Ca2+ release in ER in the skeletal muscle, thus reducing actin/myosin interaction
  • Malignant hyperthermia (and spasms)

(centrally acting muscle relaxant)

90
Q

Botulinum toxin
- MOA
- Effect

A
  • Inhibits SNARE fusion proteins
  • Prevents exocytosis of Ach : flaccid paralysis
91
Q

List of peripherally acting muscle relaxants (5)

A
  1. (cis)atracurium
  2. mivacurium
  3. pipecuronium
  4. rocuronium
  5. succinylcholine (suxamethonium)

Rocknroll AMPS

92
Q

MOA and effect of non-depolarizing peripheral muscle relaxants (Rock AMP)

A
  • Competitive antagonist of Nm Ach-R
  • Binds to the receptor instead of Ach -> no opening of ion channels -> muscle paralysis
93
Q

Indications of non depolarizing peripheral muscle relaxants (5) (Rock AMP)

A
  • Surgical narcosis
  • Artificially respirated patients
  • Intubation
  • Tetanus
  • Epilepsy
94
Q

Succinylcholine (suxamethonium)
- MOA
- Indication

A
  • Selective agonist of Nicotonic-m receptor -> depolarization blockade which cannot be stopped by Ach-esterase
  • Surgical procedures where rapid onset + brief duration is needed (intubation)

ONLY DEPOLARIZING PERIPHERAL RELAXANT

95
Q

What are the strong “mu” agonist semisynthetic opioids?

A
  • Hydromorphone
  • Oxycodone
96
Q

What are the strong “mu” agonist synthetic opioids?

A
  • Methadone
  • Meperidine
  • Fentanyl
97
Q

What are the weak “mu” agonist semisynthetic opioids?

A
  • Dihydrocodeine
98
Q

What are the weak “mu” agonist synthetic opioids?

A
  • Tramadol
  • Loperamide
  • Diphenoxylate
99
Q

What are the mixed drug semisynthetic opioids?

A
  • Buprenorphine
  • Nalbuphine
100
Q

What are the pure antagonist semisynthetic opioids?

A
  • Naloxone
  • Naltrexone
101
Q

Indications of methadone (2)

A
  • Management of opioid withdrawal syndrome
  • Maintenance programs for addicts

(Methadone kinda sounds like meth addict)

102
Q

Duration of action of meperidine?

A

2-4 hours (shorter than morphine)

103
Q

How is meperidine different from morphine?

A
  • weaker sedative
  • no antitussive effect
  • anti-muscarinic effect (increases HR)
104
Q

2 key points of fentanyl

A
  • short acting
  • 100x more potent than morphine
105
Q

Tramadol
- MOA, Effect
- Side effects (3)

A
  • Weak opoid R agonist + Inhibitor of NE + 5HT reuptake
  • Nausea, dizziness, serotonin syndrome
106
Q

What is the MOA of buprenorphine?

A

partial “mu” agonist + “k” antagonist

107
Q

Nalbuphine
- MOA
- Indication

A
  • “mu” antagonist + “k” agonist (mixed drug semisynthetic opioid)
  • Spinal anesthesia
108
Q

Indication of naloxone

A

Management of acute opioid overdose

109
Q

Indication of naltrexone

A

Management of opioid + alcohol withdrawal symptoms

110
Q

Indication of methyl-natrexone

A

Treatment of opioid induced constipation

111
Q

Nitrous oxide
- Effect
- Indications
- Side effects

A
  • Weak general anesthetic and analgesic effect
  • Carrier gas in surgical anesthesia and analgesia in dentistry, child birth
  • Teratogenic effects, megaloblastic anemia
112
Q

What are the inhalation anesthetics that are volatile liquids? (3)

A
  • Isoflurane
  • Desflurane
  • Sevoflurane
113
Q

What is the most commonly used inhaled anesthetic?

A

sevoflurane (most potent + rapid recovery)

114
Q

When is isoflurane preferred?

A

in neurosurgery -> less risk of seizures

115
Q

What are benzodiazepines used for?

A

The most frequent used sedative-hypnotics

116
Q

Benzodiazepines
- MOA
- Effects (5)
- Side effects (4)

A
  • Bind to GABA(a) receptor and promotes further GABA binding, which causes hyperpolarization (Cl) and decreased neurotransmission
  • Anxiolytic, sedative, hypnotic, muscle relaxant / antiepileptic but NO gen anesthesia
  • Sedation, mild dependance, tolerance, anterograde amnesia
117
Q

Antidote of benzodiazepines

A

Flumazenil (GABA antagonist)

118
Q

5 benzodiazepines

A
  1. Diazepam
  2. Clonazepam
  3. Alprazolam
  4. Nitrazepam
  5. Midazolam
119
Q

Dose for diazepam

A
  • 5-10mg
  • For status epilepticus iv 30mg
120
Q

Dose of alprazolam

A

Oral : 2-3x 0.25-0.5mg

121
Q

Which benzodiazepines are long acting?

A
  • Diazepam
  • Clonazepam
122
Q

Which benzodiazepines are short acting?

A
  • Nitrazepam
  • Midazolam
123
Q

What are the 5 non benzodiazepine anxiolytics & hypnotics?

A
  • Melatonin
  • Ramelteon
  • Buspirone
  • Zaleplon
  • Zolpidem
124
Q

Zaleplon, zolpidem
- MOA
- Effects (3)
- Antidote if overdose

A
  • GABA(a) agonist - high affinity to BDZ receptors with alpha1 subunits
  • Induces sleep, minimal anxiolytic and muscle relaxant (slight antiepileptic)
  • Flumazenil
125
Q

Buspirone
- MOA
- Effect

A
  • SerotoninR-1a partial agonist (Gi coupled) and non GABA-ergic anxiolytic
  • Selective anxiolytic effect, but NO sedative, hypnotic, muscle relaxant effect

(non benzo relaxant with melatonin etc)

(Think of a bus with happy kids on it)

126
Q

Melatonin and ramelteon
- MOA
- Effect

A
  • Non GABAergic hypnotics, and Ramelteon is a MT1 + MT2 agonist
  • Decrease time of sleep onset for insomnia
127
Q

What are the 1st generation “typical” antipsychotics? (3)

A
  • Haloperidol
  • Chlorpromazine
  • Droperidol
    (Helpful cheerleaders direct)
128
Q

MOA of the 1st generation antipsychotics (2)

A
  • Competitive D2 inhibitors
  • Strongly sedative, will cause EPS (extra-pyramidal symptoms)
129
Q

Indication for Haloperidol

A

Management of acute psychotic disorders (acute delirium)

130
Q

Indication for droperidol

A

Sedative effect, used in neuroleptanalgesia

131
Q

What are the 5 atypical / 2nd generation antipsychotic agents?

A
  • Risperidone
  • Olanzapine
  • Quetiapine
  • Aripiprazole
  • Clozapine

“Ranks of quarterbacks at camp”

132
Q

What is a common side effect of atypical / 2nd generation antipsychotics?

A

Metabolic syndrome (weight gain, diabetes, dislipidemia)

133
Q

What is the MOA of 2nd generation antipsychotics?

A

5-HT blockade is dominant, except for Quetiapine which is D2 antagonist

134
Q

What is the first drug of choice in schizophrenia?

A

Olanzapine (most sedative drug)

135
Q

List the tri-, tetra- and unicyclic antidepressants. (4)

A
  • Clomipradine, amitryptiline : tricyclic antidepressants
  • Maprotiline : tetracyclic
  • Bupropion : unicyclic

“Abandoned Children Mopped Busily”

136
Q

Clomipramine, amitryptiline :
- MOA
- effect
- Indication

A
  • Tricyclic antidepressants - inhibit the NE and 5-HT reuptake transporters
  • Elevate mood, improve mental alertness and increase physical activity
  • For major depression, phobia / anxiety, migraine, neuropathic pain, enuresis (involuntary urination)

(Abandoned Children —)

137
Q

What is MAO inhibitor? (Antidepressants)

A

An agent that interferes with the metabolism of amines in nerve endings, resulting in an increase in vesicular stores of NE and 5HT

138
Q

Moclobemide
- MOA
- Effect
- Indication
- Side effects
- Extra (2)

A
  • Selective and reversible MAO-a inhibitor
  • Increased NE -> hypertensive crisis
  • For depressed patients who do not respond to classic treatment (SSRIs)
  • «Cheese effect» + orthostatic hypotension, insomnia, seizures
  • Long T1/2, effect achieved after 2-4 weeks

(Part of antidepressants + MAO)

139
Q

What are the selective monoamine reuptake inhibitors? (6)

A

(SSRI)
- Fluoxetine
- Sertraline
- Citalopram
(SSNRI)
- Duloxetine
- Venlafaxine
(SNRI)
- Reboxetine

Five sexy cats do violin recitals 

140
Q

Fluoxetine, Sertraline, Citalopram
- MOA
- Indication
- Contraindication
- Side effects
- ROA

A
  • Selective serotonin reuptake inhibitors
  • Depression (active after 2 weeks), OCD, anxiety disorder, PTSD, bulemia
  • Pregnancy
  • Anxiety, nausea, paresthesia (tickling sensation), serotonin syndrome
  • Oral
141
Q

What is serotonin syndrome?

A

Increase in serotonin causes cognitive (delirium), autonomic (hypertension) and somatic (hyperthermia) symptoms

142
Q

Venlafaxine, duloxetine
- MOA
- Indication

A
  • Selective inhibition of 5HT AND NE reuptake
  • For patients who don’t respond to SSRIs, but also for neuropathy, fibromyalgia, anxiety disorders
143
Q

What is a positive of SSRIs and SSNRIs?

A

Little blocking activity at M, H1 and alpha1 receptors, so less side effects

144
Q

Reboxetine
- MOA
- Effect
- Side effects

A
  • Selective NE reuptake inhibitor (SNRI)
  • Increases mental alertness, motivation, activity
  • Dry mouth, HT, constipation

(Five sexy cats do violin recitals)

145
Q

Lithium-carbonate
- MOA
- Indication
- Side effects
- ROA
- Pharmacokinetics (2)

A
  • Prevents recycling of inositol -> decreased IP3 and DAG -> problems with GQ so less second messengers -> less neuronal activity -> mood stabilization
  • For bipolar disorders (main one)
  • Tremor, confusion, polyuria, teratogenic
  • Oral
  • Excretes into breast milk + excreted unchanged into urine

(Liberals against tinted mirrors)

146
Q

Mirtazapine
- MOA
- Effect

A
  • alpha 2 antagonist + 5HT3 and H receptor inhibition
  • Effects :
    X Increased NE synthesis and release : weight gain
    X 5HT3 inhibition : anxiolytic and antiemetic
    X H inhibition : sedative

(Liberals Against Tinted Mirrors)

147
Q

Agomelatine
- MOA
- Effect
- Contraindication
- Side effects

A
  • Melatonin Agonist and serotonin ANTAgonist
  • For recovery of circadian rythm
  • Not for dementia patients and those older than 75
  • Sedation, weight gain, liver damage, anxiety

(liberals Against tinted mirrors)
(Think about 2 gommes in ancient Rome, one is happy but covered in ants and the other is sleeping soundly)

148
Q

Tianeptine
- MOA
- Effect

A
  • Increases 5HT reuptake in the brain + modifies glutamate receptors
  • Inhibition of stress-induced activation of HPA axis (anxiolytic)

(Liberals against TINTED mirrors)

149
Q

List 8 NSAIDS

A
  • Phenylbutazone
  • Diclofenac
  • Indomethacin
  • Ibuprofen / ketoprofen
  • Naproxen
  • Metamizole
  • Meloxicam
  • Celecoxib

Past Dinnertime I Met Melancholic Indonesian Celebrities Napping

150
Q

Contraindications of NSAIDs

A
  • GI bleeding
  • Allergy, asthma
  • Impaired kidneys
  • HF
  • Pregnancy
151
Q

Ibuprofen/ketoprofen
- MOA
- Indications
- Dose

A
  • Non selective COX inhibitor (NSAID)
  • Analgesic use in children, or to close ductus arteriosus
  • Dose : 1 to 4 x 200-600mg
152
Q

Phenylbutazone
MOA
Indications (2)

A
  • NSAID
  • Gout, arthritis
153
Q

Diclofenac
- MOA
- Dose
- Indication

A
  • NSAID
  • Dose : 2-3 x 50mg
  • Chronic rheumatic pain
    (past DINNERTIME i met…)
154
Q

Indomethacin
- MOA
- Indications (3)

A
  • NSAID (inhibits COX non selectively)
  • Acute gout attacks, ductus arteriosus closure, BM suppression
155
Q

Naproxen
- MOA
- Indications (2)

A
  • NSAID (COX1 & COX2)
  • Analgesic use, weak anti-inflammatory / management of menstrual cramps
156
Q

Metamizole
- MOA
- Effect

A
  • NSAID
  • Excellent analgesic effect but weak anti-inflammatory
    (i MET melancholic indonesian celebrities)
157
Q

Celecoxib
- MOA
- Side effects (4)

A
  • COX-2 selective (reversible) inhibitor
  • Cardiovascular risk, GI irritation, renal damage, prothrombic effect
158
Q

What is a non-opioid analgesic?

A

Paracetamol (aka acetaminophen)

159
Q

Paracetamol
- MOA
- Effect
- Side effects
- Dose
- Extra

A
  • Inhibition of COX in the CNS
  • Analgesia and antipyretic, but NO anti-inflammatory or antiplatelet effect
  • Hepatotoxic, angiodema, leukocytopenia
  • 1-4 x 500-1000mg
  • Short acting : 2-3 hours
160
Q

Sumatriptan
- MOA
- Effect
- Indication
- Side effects
- ROA (3)

A
  • Selective serotonin 1B and 1D agonist
  • Vasoconstriction of vessels and prevention of release of vasoactive peptides
  • First line agent in acute migraine attack
  • Coronary vasospasm, dizziness, muscle weakness
  • Oral, inhaled, parenteral
161
Q

Treatment of trigemino-autonomic headaches

A

First line : triptans, verapamil
Second line : lithium, valproate

162
Q

Treatment of tension headaches

A

Acute : NSAIDS, paracetamol, caffeine
Prophylactic : amitryptiline, mirtazapine

163
Q

List 8 IV anesthetics

A
  • Atropine
  • Etomidate
  • Fentanyl
  • Ketamine
  • Midazolam
  • Dexmedetomidine
  • Thiopental
  • Propofol

Adventurous Elves Flaunted Kittens Meanwhile Dragons Tore Paris

164
Q

Atropine
- MOA
- Indication
- Side effects
- Dose

A
  • Non-selective muscarinic antagonist (decreases parasympathetic tone)
  • Reversal of AV block, reversal of the effect of curare type skeletal muscle relaxants, reduce salivation before surgery
  • Tachycardia, bronchodilation, mydriasis
  • 0.3-1.0mg
165
Q

Propofol
- MOA
- Indication
- Kinetics
- Side effects

A
  • Facilitation of GABA inhibition at GABA(a) receptors leads to Cl influx
  • Induction and maintenance of anesthesia + antiemetic
  • Short acting, hepatic metabolism
  • Hypotension, metabolic acidosis, overdose (MJ :c )
166
Q

Etomidate
- MOA
- Indication
- Side effects

A
  • Facilitate GABA mediation at GABA(a) receptors, causing Cl influx
  • Induction of anesthesia for patients with limited cardiac or respiratory reserve
  • Nausea, vomiting, suppression of adrenocortical stress response
167
Q

Ketamine
- MOA
- Effects
- Indication
- Side effects (4)

A
  • NMDA receptor antagonist (glutamate R)
  • Dissociative anesthesia + stimulates circulation
  • For induction of anesthesia in short interventions
  • Cardiovascular stimulant, intracranial hypertension, hallucinations, relaxes bronchi

(For SE just think about people on drugs)

168
Q

Dexmedetonidine
- MOA
- Indication

A
  • Alpha 2 agonist
  • Short term sedation in ICU + for hypertension

(IV anesthetic : dragons)

169
Q

Thiopental
- MOA
- Indication
- Side effects (4)
- Kinetics

A
  • Facilitate GABA inhibition at GABA(a) receptors, causing Cl influx
  • Induction of anesthesia, but no analgesia
  • Apnea, coughing, cardiac and respiratory depressant, cerebral vasoconstriction
  • Ultra short acting, rapid onset, but slow recovery

(Dragons tore paris)

170
Q

Midazolam
- MOA
- Indication
- Side effects

A
  • Facilitate GABA-mediated inhibition at GABA(a) receptors, causing Cl influx
  • Preoperative sedation, induction of anesthesia, outpatient anesthesia (not too strong)
  • Cardiovascular + respiratory depression
171
Q

Fentanyl
- MOA
- Indication
- Kinetics

A
  • Opioid mu-receptor agonist
  • Induction and maintenance of anesthesia
  • Strong CNS depression, works as long as it’s infused
172
Q

Antiepileptics used in partial seizures and tonic-clonic seizures (5)

A
  • Phenytoin
  • Phenobarbital
  • Pregabalin
  • Carbamazepine
  • Vigabatrin

3 very pretty chicks

173
Q

Phenytoin and Carbamazepine
- MOA
- Effect
- Indication
- Side effects (4)
- ROA

A
  • Inhibition of voltage gated Na channels
  • Prevent seizure propagation, but not initiation
  • For tonic clonic seizures and trigeminal neuralgia
  • CNS depression, osteomalacia, hirsutism, anemia
  • Oral, IV (only phenytoin)
174
Q

Phenobarbital
- MOA
- Effect
- Side effects (3)

A
  • Barbiturate : inhibition through GABA(a) receptors, and may also block Na/Ca channels
  • Prevent tonic clonic or partial seizures
  • Sedative, mental disturbance, enzyme inducer
175
Q

Pregabalin / Gabapentin
- MOA
- Indication
- Side effects (2)

A
  • Inhibits N-type Ca channels and decreases Glutamate release
  • For partial seizures and neuropathic pain
  • Drowsiness, headache
176
Q

Antiepileptics used in absence seizures specifically (2)

A
  • Ethosuximide
  • Clonazepam
177
Q

Broad spectrum antiepileptic drugs (3)

A
  • Valproate
  • Lamotrigine
  • Levetiracetam

(Ethan closely levitates valuable lamps)

178
Q

Drugs used for treatment of status epilepticus (3)

A
  • Diazepam
  • Phenytoin
  • Phenobarbital
179
Q

Ethosuximide
- MOA
- Indication
- Side effects

A
  • Inhibits T-type Ca channels in the thalamus
  • Absence seizures only!!
  • Gi symptoms, headache, dizziness
180
Q

Clonazepam
- MOA
- Effect
- Indication
- Side effects

A
  • Benzodiazepine
  • Enhances effect of GABA
  • Absence seizures, panic disorders
  • Sedation, tolerance
181
Q

Valproate
- MOA
- Effect
- Indication
- Side effects
- Extra

A
  • Inhibits Ca channels
  • Enhances GABA transmission
  • All seizures, bipolar disorders
  • Hepatotoxicity, thrombocytopenia, GI symptoms
  • Inhibits CP450 enzymes
182
Q

Lamotrigine
- MOA
- Indication
- Side effects

A
  • Inhibits Na channels + reduces glutamate release
  • Most seizures
  • Steven Johnson syndrome
183
Q

Levetiracetam
- MOA
- Indication
- Side effects

A
  • Prevents synaptic release of glutamate
  • Tonic-clonic, partial, myoclonic seizures in children
  • Aggressive behavior, insomnia
184
Q

Which antiepileptics can be given to pregnant women? (2)

A
  • Levetiracetam
  • Lamotrigine
185
Q

Vigabatrin
- MOA
- Effect
- Indication
- Side effects (3)

A
  • Inhibits GABA metabolism enzyme
  • Decreased GABA metabolism : more circulating GABA
  • Partial seizures + infantile spasms
  • Peripheral sight loss, sedation, confusion
186
Q

Ropinirole, pramipexole
- MOA
- Indication
- Side effects (3)

A
  • Dopamine D2 agonists (Gi/o)
  • Parkinson’s
  • Dyskinesia, psychosis, nausea

(Retired_prams)

187
Q

Selegiline
- MOA
- Effect
- Indication
- Side effects

A
  • Selective + reversible MAO-B inhibitor
  • Increases dopamine levels in the brain and increases activity
  • Parkinson’s, alzheimer’s
  • Same as levodopa
188
Q

Entacapone
- MOA
- Effect
- Indication

A
  • COMT inhibitor (catechol-o-methyl transferase)
  • Inhibits metabolism of levodopa
  • Parkinson’s
189
Q

Amantadine
- MOA
- Effect
- Indication
- Side effects

A
  • Antiviral drug
  • Increased dopamine release somehow
  • Parkinson’s disease
  • Pale skin, psychosis
190
Q

Drugs used to treat Parkinson’s (7)

A
  • L-dopa + carbidopa
  • Ropinirole
  • Pramipexole
  • Selegiline
  • Amantadine
  • Procyclidine

Retired car professional loves selling amazing prams

191
Q

Drugs used to treat Alzheimer’s (3)

A
  • Rivastigmine
  • Memantine
  • Piracetam
192
Q

Memantine
- MOA
- Side effects

A
  • Glutamate NMDA receptor blocker
  • Confusion, agitation
193
Q

What are 6 indirect sympathomimetics?

A
  • Ephedrine
  • Phenylephrine
  • Oxymetazoline
  • Clonidine
  • Rilmenidine
  • Methyldopa

“Cheerful rabbits often play exciting melodies.”

5. Pharmacology AC (17 decks)

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