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5. Pharmacology AC > Topic list A drugs > Flashcards

Topic list A drugs Flashcards

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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
Levodopa - MOA - Effect - Indication - Side effects (5)
- Metabolic precursor of dopamine - Increases the activity of DOPA-decarboxylase - Parkinson's disease - Dyskenia, hypotension, arrythmias, nausea, depression
26
What is the effect of carbidopa?
It inhibits DOPA-decarboxylase and prevents synthesis of dopamine peripherally
27
What is the effect of metyrosine
Inhibits synthesis of DOPA from tyrosine
28
Cholinomimetics that are direct muscarinic and/or nicotonic agonists
- carbachol - pilocarpine
29
Cholinomimetics that are indirect agonists
- Neostigmine - pyridostigmine - rivastigmine
30
Carbachol - MOA - Effect
- Muscarinic and nicotinic agonist - Miosis via ciliary muscle contraction (M3) and decreased intraocular pressure
31
What is the MOA of pilocarpine?
Direct muscarinic agonist
32
What is the effect of pilocarpine?
Increases salivation and sweat production
33
What are the indications of neostigmine and pyridostigmine?
Reverse the effects of relaxants and for treatment of myasthenia gravis
34
What is special about neostigmine and pyridostigmine?
They are quaternary amine and do not cross the BBB
35
Rivastigmine - MOA - Indication - Side effects
- Cholinesterase inhibitor - For the treatment of mild dementia of alzheimer type - Nausea, vomiting, bradycardia
36
8 examples of muscarinic antagonists (receptor blocking)
- Atropine - Butyl-scopalamine - Procyclidine - Cyclopentolate - Ipratropium - Tiotropium - Solifenacin - Oxybutinin at pro cyclist tournaments, i solely binge oxy
37
Which muscarinic receptor blocking drugs are selective?
Tiotropium, solifenacin and oxybutinin are selective M3 antagonists
38
How is butyl-scopalamine different from scopalamine?
It cannot enter the CNS
39
Procyclidine - MOA - Indications
- Muscarinic receptor antagonist - Parkinson's disease (increase in Ach due to decrease in dopamine) - Extrapyramidal disorders caused by drugs
40
Can procyclidine enter the CNS?
Yes, it has a tertiary amine
41
What is the indication of cyclopentolate?
It is used to dilate the pupils in ophtalmologic examinations
42
ipratropium and triotropium MOA Effect ROA
- Muscarinic antagonist - Bronchodilation - Inhaled from a spray
43
MOA of epinephrine (small and large dose)
- Small dose : B stimulation predominates - Big dose : A1 stimulation predominates
44
Epinephrine doses
- Anaphylaxia : 0.15-0.5mg or 0.05-0.1mg in IV - Resuscitation : 1mg IV
45
Norepinephrine - MOA - Effect - Indications
- a1, a2 and b1 agonist - Vasoconstriction - Acute hypotension in shock + cardiac arrest / complete heart block
46
MOA of dopamine (small, medium and large dose)
- small : D1 - vasodilation, increase in GFR - medium : D1, b1 - positive inotropic & chronotropic effect - large dose : a1 effect - vasoconstriction
47
Indications of dopamine (3)
- Shock - Renal insufficiency - Heart failure
48
Dobutamine - MOA - Effect
- b1 agonist - Cardiac Output and Stroke Volume increase
49
Isoprenaline - MOA - Effect - Contraindications
- Non selective b-agonist (it’s one of the catecholamines) - Positive inotropic and chronotropic effect via b1+ bronchodilation via b2 - Underlying coronary disease
50
Ephedrine MOA Indications (3)
- Indirect sympathomimetic + weak b2 agonist - Nasal decongestant + Treatment of anesthesia related hypotension + Appetite suppressant
51
Phenylephrine - MOA - Indications (3)
- a1 agonist - Hypotension, nasal decongestion, mydriasis for ophtalmologic examination
52
MOA of oxymetazoline
- Local a1 agonist - Systemic a2 agonist
53
Clonidine - MOA - Effects Indications (3)
- a2 agonist (Gi coupled - inhibitory) - Presynaptic a2R leads to decrease in release of NE and thus a decrease in BP - Hypertension, Tourette’s, ADHD
54
MOA of Rilmenidine
A2 agonist
55
Methyldopa - MOA - Extra
- A2 agonist - It can be used even during pregnancy because it can’t activate other adrenergic receptors
56
3 a1-selective antagonist drugs
- Prazosin - Doxazosin - Tamsulosin
57
Effect of prazosin, doxazosin, tamsulosin
Relax muscle of prostate + bladder neck
58
MOA of urapidil
- a1 selective antagonist - a2 agonist - b antagonist
59
Carvedilol - MOA - Indications
- a1 selective antagonist and b antagonist - Hypertension, CHF, chronic stable angina (It decreases HT through alpha and reduces tachycardia, heart problems through beta)
60
Phentolamine - MOA - Effect - Indication
- Non selective a-antagonist - Vasodilation - Treatment of pheochromocytoma & acute hypertension due to a-agonist overdose
61
4 non-selective beta antagonists
- Propanolol - Pindolol - Timolol - Sotalol
62
4 beta1-selective antagonists
- Bisoprolol - Metoprolol - Esmolol - Nebivolol
63
Indications for b1-selective antagonists
- Hypertension - Chronic stable angina - CHF
64
Dosage of metoprolol
2x25-100mg
65
Which b-selective antagonists cross the BBB?
Bisoprolol and nebivolol because they are lipophilic
66
Which local anesthetics are amides?
- Lidocaine - Articaine - Bupivacaine
67
Which local anesthetics are esters?
- Cocaine - Benzocaine
68
What is the MOA of local anesthetics?
Na+ channel blockers
69
Lidocaine - Indications (3) - Duration of action
- Local surgical procedures, post operative analgesia and ventricular arrhythmia - 1-2 hours, 2-4 hours if combined with epinephrine
70
Cocaine MOA Effect
- binds and inactivates sodium channels, which inhibits excitation - blocks NE reuptake into nerve terminals because of its vasoconstrictive properties : intrinsic sympathomimetic effect
71
Effect of benzocaine
Reversibly stabilizes the neuronal membrane - decreases its permeability to Na ions : anesthetic
72
What type of receptors are the opioid receptors?
They are all Gi coupled
73
What is the MOA of morphine?
Strong opioid receptor agonist
74
Cite 6 main effects of morphine
1. Analgesia 2. Respiratory depression 3. Decreased BP + bradycardia 4. Nausea, vomiting 5. Bronchoconstriction 6. Urinary retention & constipation
75
Dosage of morphine (per os / sc / iv)
- Per os : morphine sulfate - 2x 30-100mg - Sc : morphine hydrochloride - 10-20mg - IV : morphine hydrochloride - 1mg (repeated up to 10mg)
76
Codeine - MOA - Effects
- Weak agonist of MOR - mu opioid receptor - Antitussive and weak analgesic effect
77
Aspirin / acetylsalicilic acid - MOA - Effect - Side effects (4)
- 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
78
Dose-dependant effects of acetylsalicilic acid
- 50-200mg/day : inhibition of platelet aggregation - 500mg/day : analgesic and antipyretic - 4-5g/day : anti-inflammatory
79
What drug is used for management of acute gout attacks?
Colchicine
80
Colchicine - MOA - Side effects (3)
- Microtubule assembly inhibitor -> inhibits mitosis - Hepatotoxic, Neurotoxic, Nephrotoxic
81
Drugs used for management of chronic gout
1. Allopurinol 2. Rasburicase
82
MOA of allopurinol
Uric acid synthesis inhibitor
83
MOA of rasburicase
Recombinant type of urate oxidase : decreases serum uric acid by transforming uric acid into allantoin
84
List of centrally acting muscle relaxants (6) aka spasmolytics
1. Diazepam 2. Baclofen 3. Tizanidine 4. Tolperisone 5. Dantrolene 6. Botulinum toxin (2B2D2T acronym)
85
Diazepam - MOA - Effect - Indications - Dosage
- 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
Baclofen - MOA - Effect
- GABA(b) receptor agonist - Gi coupled receptor -> K+ efflux -> hyperpolarization -> long lasting muscle relaxant
87
Tizanidine - MOA - Effect
- alpha 2 agonist (Gi coupled) - causes pre-synaptic stimulation of alpha 2 R -> inhibition of glutamate release -> muscle relaxation
88
MOA and effect of tolperisone
- MOA is unknown - Causes reduction of the muscle reflex
89
Dantrolene - MOA - Effect - Indications
- 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
Botulinum toxin - MOA - Effect
- Inhibits SNARE fusion proteins - Prevents exocytosis of Ach : flaccid paralysis
91
List of peripherally acting muscle relaxants (5)
1. (cis)atracurium 2. mivacurium 3. pipecuronium 4. rocuronium 5. succinylcholine (suxamethonium) Rocknroll AMPS
92
MOA and effect of non-depolarizing peripheral muscle relaxants (Rock AMP)
- Competitive antagonist of Nm Ach-R - Binds to the receptor instead of Ach -> no opening of ion channels -> muscle paralysis
93
Indications of non depolarizing peripheral muscle relaxants (5) (Rock AMP)
- Surgical narcosis - Artificially respirated patients - Intubation - Tetanus - Epilepsy
94
Succinylcholine (suxamethonium) - MOA - Indication
- 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
What are the strong "mu" agonist semisynthetic opioids?
- Hydromorphone - Oxycodone
96
What are the strong "mu" agonist synthetic opioids?
- Methadone - Meperidine - Fentanyl
97
What are the weak "mu" agonist semisynthetic opioids?
- Dihydrocodeine
98
What are the weak "mu" agonist synthetic opioids?
- Tramadol - Loperamide - Diphenoxylate
99
What are the mixed drug semisynthetic opioids?
- Buprenorphine - Nalbuphine
100
What are the pure antagonist semisynthetic opioids?
- Naloxone - Naltrexone
101
Indications of methadone (2)
- Management of opioid withdrawal syndrome - Maintenance programs for addicts (Methadone kinda sounds like meth addict)
102
Duration of action of meperidine?
2-4 hours (shorter than morphine)
103
How is meperidine different from morphine?
- weaker sedative - no antitussive effect - anti-muscarinic effect (increases HR)
104
2 key points of fentanyl
- short acting - 100x more potent than morphine
105
Tramadol - MOA, Effect - Side effects (3)
- Weak opoid R agonist + Inhibitor of NE + 5HT reuptake - Nausea, dizziness, serotonin syndrome
106
What is the MOA of buprenorphine?
partial "mu" agonist + "k" antagonist
107
Nalbuphine - MOA - Indication
- "mu" antagonist + "k" agonist (mixed drug semisynthetic opioid) - Spinal anesthesia
108
Indication of naloxone
Management of acute opioid overdose
109
Indication of naltrexone
Management of opioid + alcohol withdrawal symptoms
110
Indication of methyl-natrexone
Treatment of opioid induced constipation
111
Nitrous oxide - Effect - Indications - Side effects
- Weak general anesthetic and analgesic effect - Carrier gas in surgical anesthesia and analgesia in dentistry, child birth - Teratogenic effects, megaloblastic anemia
112
What are the inhalation anesthetics that are volatile liquids? (3)
- Isoflurane - Desflurane - Sevoflurane
113
What is the most commonly used inhaled anesthetic?
sevoflurane (most potent + rapid recovery)
114
When is isoflurane preferred?
in neurosurgery -> less risk of seizures
115
What are benzodiazepines used for?
The most frequent used sedative-hypnotics
116
Benzodiazepines - MOA - Effects (5) - Side effects (4)
- 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
Antidote of benzodiazepines
Flumazenil (GABA antagonist)
118
5 benzodiazepines
1. Diazepam 2. Clonazepam 3. Alprazolam 4. Nitrazepam 5. Midazolam
119
Dose for diazepam
- 5-10mg - For status epilepticus iv 30mg
120
Dose of alprazolam
Oral : 2-3x 0.25-0.5mg
121
Which benzodiazepines are long acting?
- Diazepam - Clonazepam
122
Which benzodiazepines are short acting?
- Nitrazepam - Midazolam
123
What are the 5 non benzodiazepine anxiolytics & hypnotics?
- Melatonin - Ramelteon - Buspirone - Zaleplon - Zolpidem
124
Zaleplon, zolpidem - MOA - Effects (3) - Antidote if overdose
- GABA(a) agonist - high affinity to BDZ receptors with alpha1 subunits - Induces sleep, minimal anxiolytic and muscle relaxant (slight antiepileptic) - Flumazenil
125
Buspirone - MOA - Effect
- 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
Melatonin and ramelteon - MOA - Effect
- Non GABAergic hypnotics, and Ramelteon is a MT1 + MT2 agonist - Decrease time of sleep onset for insomnia
127
What are the 1st generation "typical" antipsychotics? (3)
- Haloperidol - Chlorpromazine - Droperidol (Helpful cheerleaders direct)
128
MOA of the 1st generation antipsychotics (2)
- Competitive D2 inhibitors - Strongly sedative, will cause EPS (extra-pyramidal symptoms)
129
Indication for Haloperidol
Management of acute psychotic disorders (acute delirium)
130
Indication for droperidol
Sedative effect, used in neuroleptanalgesia
131
What are the 5 atypical / 2nd generation antipsychotic agents?
- Risperidone - Olanzapine - Quetiapine - Aripiprazole - Clozapine “Ranks of quarterbacks at camp”
132
What is a common side effect of atypical / 2nd generation antipsychotics?
Metabolic syndrome (weight gain, diabetes, dislipidemia)
133
What is the MOA of 2nd generation antipsychotics?
5-HT blockade is dominant, except for Quetiapine which is D2 antagonist
134
What is the first drug of choice in schizophrenia?
Olanzapine (most sedative drug)
135
List the tri-, tetra- and unicyclic antidepressants. (4)
- Clomipradine, amitryptiline : tricyclic antidepressants - Maprotiline : tetracyclic - Bupropion : unicyclic “Abandoned Children Mopped Busily”
136
Clomipramine, amitryptiline : - MOA - effect - Indication
- 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
What is MAO inhibitor? (Antidepressants)
An agent that interferes with the metabolism of amines in nerve endings, resulting in an increase in vesicular stores of NE and 5HT
138
Moclobemide - MOA - Effect - Indication - Side effects - Extra (2)
- 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
What are the selective monoamine reuptake inhibitors? (6)
(SSRI) - Fluoxetine - Sertraline - Citalopram (SSNRI) - Duloxetine - Venlafaxine (SNRI) - Reboxetine Five sexy cats do violin recitals 
140
Fluoxetine, Sertraline, Citalopram - MOA - Indication - Contraindication - Side effects - ROA
- Selective serotonin reuptake inhibitors - Depression (active after 2 weeks), OCD, anxiety disorder, PTSD, bulemia - Pregnancy - Anxiety, nausea, paresthesia (tickling sensation), serotonin syndrome - Oral
141
What is serotonin syndrome?
Increase in serotonin causes cognitive (delirium), autonomic (hypertension) and somatic (hyperthermia) symptoms
142
Venlafaxine, duloxetine - MOA - Indication
- Selective inhibition of 5HT AND NE reuptake - For patients who don’t respond to SSRIs, but also for neuropathy, fibromyalgia, anxiety disorders
143
What is a positive of SSRIs and SSNRIs?
Little blocking activity at M, H1 and alpha1 receptors, so less side effects
144
Reboxetine - MOA - Effect - Side effects
- Selective NE reuptake inhibitor (SNRI) - Increases mental alertness, motivation, activity - Dry mouth, HT, constipation (Five sexy cats do violin recitals)
145
Lithium-carbonate - MOA - Indication - Side effects - ROA - Pharmacokinetics (2)
- 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
Mirtazapine - MOA - Effect
- 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
Agomelatine - MOA - Effect - Contraindication - Side effects
- 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
Tianeptine - MOA - Effect
- Increases 5HT reuptake in the brain + modifies glutamate receptors - Inhibition of stress-induced activation of HPA axis (anxiolytic) (Liberals against TINTED mirrors)
149
List 8 NSAIDS
- Phenylbutazone - Diclofenac - Indomethacin - Ibuprofen / ketoprofen - Naproxen - Metamizole - Meloxicam - Celecoxib Past Dinnertime I Met Melancholic Indonesian Celebrities Napping
150
Contraindications of NSAIDs
- GI bleeding - Allergy, asthma - Impaired kidneys - HF - Pregnancy
151
Ibuprofen/ketoprofen - MOA - Indications - Dose
- Non selective COX inhibitor (NSAID) - Analgesic use in children, or to close ductus arteriosus - Dose : 1 to 4 x 200-600mg
152
Phenylbutazone MOA Indications (2)
- NSAID - Gout, arthritis
153
Diclofenac - MOA - Dose - Indication
- NSAID - Dose : 2-3 x 50mg - Chronic rheumatic pain (past DINNERTIME i met...)
154
Indomethacin - MOA - Indications (3)
- NSAID (inhibits COX non selectively) - Acute gout attacks, ductus arteriosus closure, BM suppression
155
Naproxen - MOA - Indications (2)
- NSAID (COX1 & COX2) - Analgesic use, weak anti-inflammatory / management of menstrual cramps
156
Metamizole - MOA - Effect
- NSAID - Excellent analgesic effect but weak anti-inflammatory (i MET melancholic indonesian celebrities)
157
Celecoxib - MOA - Side effects (4)
- COX-2 selective (reversible) inhibitor - Cardiovascular risk, GI irritation, renal damage, prothrombic effect
158
What is a non-opioid analgesic?
Paracetamol (aka acetaminophen)
159
Paracetamol - MOA - Effect - Side effects - Dose - Extra
- 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
Sumatriptan - MOA - Effect - Indication - Side effects - ROA (3)
- 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
Treatment of trigemino-autonomic headaches
First line : triptans, verapamil Second line : lithium, valproate
162
Treatment of tension headaches
Acute : NSAIDS, paracetamol, caffeine Prophylactic : amitryptiline, mirtazapine
163
List 8 IV anesthetics
- Atropine - Etomidate - Fentanyl - Ketamine - Midazolam - Dexmedetomidine - Thiopental - Propofol Adventurous Elves Flaunted Kittens Meanwhile Dragons Tore Paris
164
Atropine - MOA - Indication - Side effects - Dose
- 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
Propofol - MOA - Indication - Kinetics - Side effects
- 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
Etomidate - MOA - Indication - Side effects
- 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
Ketamine - MOA - Effects - Indication - Side effects (4)
- 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
Dexmedetonidine - MOA - Indication
- Alpha 2 agonist - Short term sedation in ICU + for hypertension (IV anesthetic : dragons)
169
Thiopental - MOA - Indication - Side effects (4) - Kinetics
- 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
Midazolam - MOA - Indication - Side effects
- 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
Fentanyl - MOA - Indication - Kinetics
- Opioid mu-receptor agonist - Induction and maintenance of anesthesia - Strong CNS depression, works as long as it's infused
172
Antiepileptics used in partial seizures and tonic-clonic seizures (5)
- Phenytoin - Phenobarbital - Pregabalin - Carbamazepine - Vigabatrin 3 very pretty chicks
173
Phenytoin and Carbamazepine - MOA - Effect - Indication - Side effects (4) - ROA
- 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
Phenobarbital - MOA - Effect - Side effects (3)
- 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
Pregabalin / Gabapentin - MOA - Indication - Side effects (2)
- Inhibits N-type Ca channels and decreases Glutamate release - For partial seizures and neuropathic pain - Drowsiness, headache
176
Antiepileptics used in absence seizures specifically (2)
- Ethosuximide - Clonazepam
177
Broad spectrum antiepileptic drugs (3)
- Valproate - Lamotrigine - Levetiracetam (Ethan closely levitates valuable lamps)
178
Drugs used for treatment of status epilepticus (3)
- Diazepam - Phenytoin - Phenobarbital
179
Ethosuximide - MOA - Indication - Side effects
- Inhibits T-type Ca channels in the thalamus - Absence seizures only!! - Gi symptoms, headache, dizziness
180
Clonazepam - MOA - Effect - Indication - Side effects
- Benzodiazepine - Enhances effect of GABA - Absence seizures, panic disorders - Sedation, tolerance
181
Valproate - MOA - Effect - Indication - Side effects - Extra
- Inhibits Ca channels - Enhances GABA transmission - All seizures, bipolar disorders - Hepatotoxicity, thrombocytopenia, GI symptoms - Inhibits CP450 enzymes
182
Lamotrigine - MOA - Indication - Side effects
- Inhibits Na channels + reduces glutamate release - Most seizures - Steven Johnson syndrome
183
Levetiracetam - MOA - Indication - Side effects
- Prevents synaptic release of glutamate - Tonic-clonic, partial, myoclonic seizures in children - Aggressive behavior, insomnia
184
Which antiepileptics can be given to pregnant women? (2)
- Levetiracetam - Lamotrigine
185
Vigabatrin - MOA - Effect - Indication - Side effects (3)
- Inhibits GABA metabolism enzyme - Decreased GABA metabolism : more circulating GABA - Partial seizures + infantile spasms - Peripheral sight loss, sedation, confusion
186
Ropinirole, pramipexole - MOA - Indication - Side effects (3)
- Dopamine D2 agonists (Gi/o) - Parkinson's - Dyskinesia, psychosis, nausea (Retired_prams)
187
Selegiline - MOA - Effect - Indication - Side effects
- Selective + reversible MAO-B inhibitor - Increases dopamine levels in the brain and increases activity - Parkinson's, alzheimer's - Same as levodopa
188
Entacapone - MOA - Effect - Indication
- COMT inhibitor (catechol-o-methyl transferase) - Inhibits metabolism of levodopa - Parkinson's
189
Amantadine - MOA - Effect - Indication - Side effects
- Antiviral drug - Increased dopamine release somehow - Parkinson's disease - Pale skin, psychosis
190
Drugs used to treat Parkinson's (7)
- L-dopa + carbidopa - Ropinirole - Pramipexole - Selegiline - Amantadine - Procyclidine Retired car professional loves selling amazing prams
191
Drugs used to treat Alzheimer's (3)
- Rivastigmine - Memantine - Piracetam
192
Memantine - MOA - Side effects
- Glutamate NMDA receptor blocker - Confusion, agitation
193
What are 6 indirect sympathomimetics?
- Ephedrine - Phenylephrine - Oxymetazoline - Clonidine - Rilmenidine - Methyldopa "Cheerful rabbits often play exciting melodies."

5. Pharmacology AC (17 decks)

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