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Medicine > BB Pharmacology NEW > Flashcards

BB Pharmacology NEW Flashcards

1
Q

Rasagiline

Selegiline

A

Dopaminergic Drugs
Type: Affects Dopamine Inactivation

Class: MOAb Inhibitors

Stop dopamine from being degraded in the pre-synaptic neurons (Conversion from dopamine to DOPAC) + protect residual dopamine vs oxidation

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2
Q

Entacapone

Tolcapone

A

Dopaminergic Drugs
Type: Affects Dopamine Inactivation

Class: COMT Inhibitors

Stop dopamine degradation from DOPAC to Homovanillic acid.
(!) May alleviate dystonias and motor fluctuations in long-term management of L-DOPA, as well as prolonging the effect on L-DOPA.

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3
Q

Benzhexol

Benztropine

A

Dopaminergic Drugs
Type: Affects Dopamine Inactivation

Class: Antimuscarinic Drugs

Antagonists of muscarinic acetylcholine receptors (mAchRs). They increase dopamine release, inhibit dopamine re-uptake, inhibit overactivity.
Side Effects: dry mouth, flushed (hot) skin, dilation of pupils, tachycardia etc…

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4
Q

Reserpine

Tetrabenazine

A

Dopaminergic Drugs
Class: Affecting Dopamine Storage

Drug: Decreasing Release

Inhibits the vesicular storage of dopamine by irreversibly inhibiting the vesicular monoamine transporter VMAT2 (used in Huntington’s).

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5
Q

Amantadine

A

Dopaminergic Drugs
Type: Affecting Dopamine Storage

Class: Increasing Release

Inhibition of amine uptake, inhibition of MOA activity, release of dopamine (and noradrenaline) from monoaminergic terminals.

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6
Q

Alpha methyl-p-tyrosine

A

Dopaminergic Drugs
Type: Affecting Dopamine Synthesis

Competitive inhibitor of dopamine: blocks dopamine synthesis by inhibiting tyrosine hydroxylase (rate-limiting step in synthesis of dopamine)

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7
Q

L-DOPA/Levadopa
Madopar (has PDCI* Benserazide)
carbidopa is another PDCI

Peripheral Decarboxylase Inhibitor

A

Dopaminergic Drugs
Type: Affecting Dopamine Synthesis

Dopaminergic nerve fibres take up L-DOPA. Converted by the enzyme DOPA decarboxylase to dopamine.

Contains peripheral decarboxylase inhibitor along with L-DOPA to prevent the conversion to dopamine to occur outside the BBB (causes nausea/vomiting due to stimulation of the chemoreceptor trigger zone).

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8
Q

Pergolide

Quinpirole

A

Dopaminergic Drugs
Type: Post Synaptic Dopamine Receptor Agonists

Show little selectivity between D1 and D2 families of receptors.

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9
Q

Bromocriptine

A

Dopaminergic Drugs
Type: Post Synaptic Dopamine Receptor Agonists

Much higher affinity for D1 than D2, also used for other types of infertility.

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10
Q

Apomorphine

A

Dopaminergic Drugs
Type: Post Synaptic Dopamine Receptor Agonists

Non-selective potent emetic: that can be given as infusion.

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11
Q

Rotigotine (!)

ropinirole, pramipexole

A

Dopaminergic Drugs
Type: Post Synaptic Dopamine Receptor Agonists

Non-selective: which has recently been introduced. It can be given as a transdermal patch (continuous administration over 24hrs)

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12
Q 
Chlorpromazine
Haloperidol
Spiperone
Sulpiride
Clozapine
A

Dopaminergic Drugs
Type: Post Synaptic Dopamine Receptor Antagonists

Drugs are used to treat schizophrenia (higher affinities for D2 then D1).

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13
Q

Paracetamol

A

Class: Treatment of Pain (Non-Opioids)

Drug: Analgesic

Anti-pyretic (anti-fever) and analgesic but little anti-inflammatory effects.

• Prevents pain: stopping prostaglandin synthesis in the CNS = through decreasing prostaglandin E2-induced reduction of glycine inhibition of spinal cord cells  endogenous spinal inhibitory mechanisms: normal.
o Decreased glycine.
• Inhibit reuptake of endogenous cannabinoids from synaptic cleft = increases effect on antinociception.

Nausea and GI Bleeding.

Ineffective as Anti-Inflammatory:
• Reduces the active oxidised form of COX-2, preventing it from forming pro-inflammatory stimuli (e.g. prostaglandins/thromboxanes).
• BUT: in the presence of peroxides (exist at sites of inflammation) mechanisms becomes inefficient (COX-2 oxidisation by peroxides).

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14
Q

Ibuprofen

A

Class: Treatment of Pain (Non-Opioids)

Drug: NSAIDs

MOA:
Mild to moderate pain.
Both analgesic and anti-inflammatory.
• Inhibits the activity of COX-1 and COX-2 enzymes.
• Decreases prostaglandin formation, recruitment of leucocytes.
• Reduces sensitisation by these inflammatory mediators.
• (!) Also travel across the BBB to have effects on the prostaglandin synthesis in the CNS.

Side Effects/Notes
Related to inhibition of COX-1.
• COX-1 regulates production of prostaglandins in the GI tract (protect the mucosa).
• Long-term use of NSAIDs can lead to peptic ulcers.

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15
Q

Diclofenac

A

Class: Treatment of Pain (Non-Opioids)

Drug: NSAIDs

MOA:
Moderate to Severe Pain
Inhibit the formation of prostaglandins.

(!) Longer acting vs ibuprofen.
• Analgesic efficacy comparable to low-dose opioids.

Due to additional activity of inhibiting phospholipase A2 and reductions in arachidonic acid (needed for synthesis of prostaglandins and leukotrienes).

Side Effects/Notes:
• Lower COX-1 selectivity: reduces the risk of GI complications.
• Higher risk of CV complications due to inhibition of endothelial prostacyclin but not thromboxane.
• Therefore, contraindicated in people with IHD and strokes.

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16
Q

Rofecoxib

A

Class: Treatment of Pain (Non-Opioids)

Drug: NSAIDs

MOA:
Selective for COX-2 Inhibitors.

Side Effects/Notes:
Nausea and GI bleeding.

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17
Q

Amitriptyline

A

Class: Treatment of Pain (Non-Opioids)

Drug: TCA

MOA:
Often described for neuropathic pain as depression and insomnia are common complications.

  • Inhibit reuptake of amines.
  • Mainly 5-HT vs noradrenaline (SNRI).
  • Inhibits sodium channels, L-type Ca2+ channels and subtypes of K+ channels and acts on NMDA receptors.
  • Has affinity for various other receptors e.g. H1, muscarinic alpha-1 and alpha-2 adrenoceptors (cause of side effects)
Side Effects/Notes:
•	Weight gain 
•	Appetite changes. 
•	Muscle stiffness, constipation, urinary retention, dry mouth (muscarinic effects). 
•	Postural Hypotension (adrenergic)
•	Nausea nervousness, dizziness.

Side effects due to anticholinergic activity (inhibition of acetylcholine muscarinic receptors, acetylcholine adrenergic receptors etc…).

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18
Q

Pregabalin

A

Class: Treatment of Pain (Non-Opioids)

Drug: Anticonvulsants

MOA:
Beneficial after 1 week of treatment.
• Binding to alpha2 delta 1 subunit of N-type voltage gated calcium channels.
•  reduction in Ca2+ entry = decreased release of neurotransmitters (glutamate, noradrenaline etc…).

(!) Alpha 2 delta 1 subunits increased in some neuropathic conditions.

Side Effects/Notes:
More Common.
• Drowsiness, dizziness and headaches

Less Common
• Peripheral oedema, visual problems, weight gain, confusion.

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19
Q

Tramadol

A

Class: Treatment of Pain (Opioids and Opioid-Like)

Drug: Atypical Opioids

MOA:
Moderate to severe pain.
Anti-nociceptive/antihyperalgesic.

  • Acts on mu opioid receptors
  • Interacts with monoaminergic systems (inhibits serotonin and noradrenaline uptake, but not as good as tricyclic antidepressants).

Vs. Opioids: improved side effect profile, reduced abuse potential, lack of tolerance and dependence.

Side Effects/Notes:
•	Nausea
•	Vomiting
•	Sweating
•	Itching 
•	Constipation

Side effects due to anticholinergic activity (action on acetylcholine muscarinic receptors).

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20
Q

Morphine

Fentanyl

A

Type: Treatment of Pain (Opioids and Opioid-Like)

Class: Typical Opioids

MOA:
Stimulate Mu Opioid Receptors
• Decreased neuronal excitability (by increasing K+ conductance) and decreased release of neurotransmitters (decreases Ca2+ influx).

Descending Inhibitory pathways
• Stimulate the periaqueductal gray (decreases pain efferent pathways)
• Inhibit the substantia gelatinosa of the SC. (Lamina II: where interneurons are.

Limbic System
• Reduces the anxiety of pain.

Side Effects/Notes:
• Paradoxically increased sensitivity to pain.
• Constipation, nausea, respiratory, depression and sleepiness.

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21
Q

Phenytoin
Carbamazepine
Sodium Valproate

A

Type: Anti-Epileptic

Class: Sodium Channels

 Bind to the inner pore of the sodium channel in its inactivated state (immediately after depolarization). (!) Zero order kinetics seen in phenytoin.
 Leads to an increased refractory period (delay in time taken to return to resting state) (!) Carbamazepine: liver enzyme induction.

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22
Q 
Ethosuximide (used in absence seizures)
Zonasamide
Carbamazepine (NOT ABSENCE SEIZURES)
Phenytoin (NOT ABSENCE SEIZURES)
Topiramate 
Lamotrigine
A

Type: Anti-Epileptic

Class: Calcium Channels

  • T-type calcium channels: require less depolarization to be activated.
  • L-type calcium channels: allow post-depolarization calcium influx and are slowly inactivated. Inhibiting these channels causes inhibition of calcium influx post-depolarization.

 N and P/Q-type channels: expressed at presynaptically (buttons).
 Mediate calcium entry for neurotransmitter release.

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23
Q

Topiramate (EXTRA)

A

Type: Anti-Epileptic

Class: Calcium Channels

also increases GABA transmission and inhibits glutamate and works on sodium channels

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24
Q

Lamotrigine (EXTRA)

A

Type: Anti-Epileptic

Class: Calcium Channels

inhibition of glutamate release as well as target in sodium channels (inner pore binding)

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25
Q

Stages of the Analgesic Ladder

A

1) Non-opioids
2) Moderate efficacy opioids
+/- non-opioids and adjuvant therapy
3) High efficacy opioids
+/- non-opioids and adjuvant therapy

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26
Q

Treatment for Neuropathic Pain

A
  1. Offer anticonvulsant (pregabalin) or tricyclic antidepressant (amitriptyline).
    a. Also: duloxetine (SNRI), gabapeptin (calcium channel ligands.).
  2. Try switching if initial drug is not tolerance.
  3. Consider tramadol (opioid agonist) only if acute rescue theraphy is needed.
  4. If oral treatment not tolerated: consider capsaicin cream.
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27
Q

Treatment for Complex Pain

A
  • Vanilloid receptor agonists (capsaicin)
  • NMDA glutamate receptor antagonists (ketamine)
  • GABAB receptor agonists (baclofen)
  • Local Anesthetics.
28
Q

Local Anaesthetics

A

• Blockage of sodium channels (e.g. lignocaine, prilocaine) i.e, the caines.
o (!) Risk of systemic toxicity: hypotension, respiratory depression.
• Administered through surface, infiltration, epidural.

29
Q

General Anaesthetics

A

• Activation of inhibitory receptors/inhibition of excitatory receptors.
o Induce CV depression (why it is monitored in surgery.

30
Q

Levetiracetam

A

Type: Anti-Epileptic

Class: Calcium Channels

• Binds to synaptic vesicle glycoprotein, SV2A and inhibits presynaptic calcium channels, reducing neurotransmitter release.

31
Q

Gabapentin

A

Type: Anti-Epileptic

Class: Calcium Channels

• Block Alpha 2 Delta 1 subunits of N-type calcium channels.

32
Q

Benzodiazepines
(Clonazepam: also, used in sedation)
Lorazepam + Diazepam

A

Type: Anti-Epileptic

Class: GABAa Receptor

 Expressed post-synaptically, lead to fast inhibitory transmission (hyperpolarization) through influx of Cl- (higher extracellularly than intracellularly).
 Stops propagation of electrical activity in cerebral cortex.
 Acts as a positive modulator by increasing frequency of receptor opening.

33
Q

Barbiturates (Phenobarbitone)

A

Type: Anti-Epileptic

Class: GABA Modulation

 Acts as a positive modulated by prolonged receptor opening and therefore more hyperpolarization.
 At high concentration: directly activates the channels which causes an anaesthetic effect.
 Liver enzyme induction.

34
Q

Vigabatrin

A

Type: Anti-Epileptic

Class: GABA Modulation

• Synthesis: inhibits GABA Transaminase leads to an increase in GABA levels (increased GABA desensitises GABA autoreceptors, reducing inhibitory feedback on release).

35
Q

Ondanzatron

Tiagabine

A

Type: Anti-Epileptic

Class: GABA Modulation

• Uptake: Inhibits GAT-1 (transporter involved in removing GABA from the synaptic cleft).

36
Q

Perampanel

Felbamate

A

Type: Anti-Epileptic

Class: Glutamate Receptors

• Antagonist of AMPA receptors/NDMA (involved in channels that are permeable to sodium ions).

37
Q 
Drugs for:
focal seizures with or without secondary generalisation
Tonic-clonic seizures
Absence seizures
Myoclonic seizures
A

focal seizures with or without secondary generalisation: carbamazepine, Iamotrigine, sodium valporate

Tonic-clonic seizures: carbamazepine, Iamotrigine, sodium valporate

Absence seizures: ethosuximide, sodium valporate

Myoclonic seizures: clonazepam, levetiracetam, sodium valporate

38
Q

Benzodiazepines

A

Type: Alcohol addiction

MOA: direct GABA agonists.

Indications:
• Withdrawal symptoms
• Seizures (prevention/treatment)
• Delirium (prevention/treatment)

39
Q

AED (Carbamazepine):

A

Type: Alcohol addiction

MOA: GABA promoters

Indications:
• Withdrawal Symptoms
• Seizure prevention

40
Q

Accamprosate

A

Type: Alcohol addiction

MOA: effect on glutamate receptors that reduce withdrawal related neuronal excitation.

Indications:
• Maintenance of abstinence

41
Q

Naltrexone

A

Type: Alcohol addiction

MOA: opioid antagonists

Indications:
• Maintenance of abstinence

42
Q

Disulfiram

A

Type: Alcohol addiction

MOA: aldehyde dehydrogenase inhibitor that allows buildup of aldehyde (makes people feel bad).

Indications:
• Maintenance of abstinence

43
Q

SSRIs (Selective Serotonin Reuptake Inhibitors)

A

Type: Alcohol addiction

Indications:
• Maintenance of abstinence
• Treatment of co-morbid depression

44
Q

Thiamine

A

Type: Alcohol addiction

Indications:
• Prevention of neurological symptoms.
• Treatment of Wernicke’s encephalopathy.

45
Q

Nalmefene

A

Type: Alcohol addiction

Indications:
• Used for reduction of alcohol consumption.

46
Q

Nicotine Replacement Theraphy

A

Type: Nicotine addiction

MOA: nicotine agonist

Indications:
• Smoking cessation

47
Q

Bupropion

A

Type: Nicotine addiction

MOA: monoamine (especially dopamine) reuptake inhibitor.

Indications:
• Smoking cessation

48
Q

Varencicline

A

Type: Nicotine addiction

MOA: Alpha-4 Beta-3 selective partial agonist of nicotinic receptors.

Indications:
• Has adverse effects (nausea and psychiatric disturbances).

49
Q

Methadone

A

Type: Opiate addiction

MOA: opioid agonist

Indications:
• Withdrawal symptoms

50
Q

Buprenorphine

A

Type: Opiate addiction

MOA: opioid mu receptor partial agonist, kappa antagonist

Indications:
• Withdrawal symptoms

51
Q

Clonidine

Lofexidine

A

Type: Opiate addiction

MOA: alpha 2 adrenoceptor agonists

Indications:
• Withdrawal symptoms

52
Q

Naltrexone

A

Type: Opiate addiction

Indications:
• Relapse prevention in selected patients.

(overdose of heroin)

53
Q 
Clomipramine
Imipramine
Desipramine
Amitriptyline
Nortriptyline
Protriptyline
A

Type: Antidepressants

Class: Tricyclic Antidepressants
(TCAs)

• Inhibit reuptake of amines.
o Different degree of selectivity for amines between them (mainly 5-HT vs noradrenaline).
• Have affinity for various other receptors e.g. H1, muscarinic alpha-1 and alpha-2 adrenoceptors.
• Dangerous in overdose (cardiotoxicity).
• Adverse effects: dry mouth, constipation, urinary retention, weight gain, postural hypotension, sedation etc…

54
Q

Phenelzine
Tranylcypromine
Iproniazid

A

Type: Antidepressants

Class: Monoamine Oxidase Inhibitors

• Irreversible Inhibition of MOA
• Non-selective MOAA versus MOAB.
• Cheese effect: tyramine (found in various cheese, red wine, beer etc…) is metabolised by MOA. Build up if inhibited.
o Causes severe headaches/hypertensive crisis.
• Interacts with pethidine (painkiller) and sympathomimetics.
• Hepatotoxicity.
Used in treatment of atypical depression (with anxiety, phobia and hypochondria).

55
Q

Moclobemide

A

Type: Antidepressants

Class: Reversible Monoamine Oxidase Inhibitors (RIMA)

• Increased selectivity for MOAA
• SAFER than irreversible MOAIs
o (!) Can switch to another medication almost immediately while in MOAs must wait.
• Higher efficacy vs MOAIs.
• Adverse Effects: nausea, agitation, confusion.

56
Q

Citalopram (active enantiomer is escitalopram
Fluoxetine
Paroxetine
Sertraline

A

Type: Antidepressants

Class: Selective Serotonin Reuptake Inhibitors (SSRIs)

• Increased selectivity for serotonin reuptake
o (!) Citalopram the most selective: longer time for serotonin to be removed from synaptic cleft.
• NO anticholinergic activity.
• NO cardiotoxic effects.
• SAFE in overdose.
• Adverse Effects: nausea, headaches, gastrointestinal problems, increased aggression, insomnia, anxiety, sexual dysfunction.
o Serotonin is released from platelets (vasoconstriction)

57
Q

Venlafaxine

A

Type: Antidepressants

Class: Serotonin Noradrenaline Reuptake Inhibitors (SNRI)

• Like TCAs: block monoamine re-uptake BUT they have no affinity for other targets (responsible for adverse effects).

58
Q

Reboxetine

A

Type: Antidepressants

Class: Noradrenaline Reuptake Inhibitors (NARI).

• Block noradrenaline re-uptake. Limited in mild depression

59
Q

Trazodone

A

Type: Antidepressants

Class: Serotonin Antagonist and Reuptake Inhibitor (SARI)

• Antagonism at 5-HT2 and alpha2 adrenergic receptors.

60
Q

Mirtazapine

A

Type: Antidepressants

Class: Noradrenergic and Specific Serotonergic Antidepressants (NaSSA)

  • Antagonist at alpha-2 adrenergic receptors
  • Affinity for histamine H1 receptors (causes drowsiness)
  • Exert antagonist effects at 5HT2 and 5HT3 receptors.
  • Adverse Effects: sedation, dry mouth, constipation
61
Q

Tianeptine

A

Type: Antidepressants

Class: Atypical Antidepressants

• Acts as an enhancer of serotonin re-uptake, but also has affinity at NMDA/AMPA glutamate receptors

62
Q

Clonazepam
Alprazolam
Lorazepam
Diazepam

A

Type: Anxiolytics

Class: Benzodiazepines

Benzodiazepines: positive allosteric modulators of GABA
• E.g. Diazepam potentiates GABA-induced hyperpolarization.
o Open state frequency increases.
o Open duration increases.

NOTE: use of flumazenil in overdose (acts as antagonist of benzodiazepine binding sides).

63
Q

Buspirone

Ipsapirone

A

Type: Anxiolytics

Class: 5-HT(1a) Agonists

64
Q

Fluoxetine
Escitalopram
Paroxetine

A

Type: Anxiolytics

Class: SSRIs

• Increased selectivity for serotonin reuptake
o (!) Citalopram the most selective: longer time for serotonin to be removed from synaptic cleft.
• NO anticholinergic activity.
• NO cardiotoxic effects.
• SAFE in overdose.
• Adverse Effects: nausea, headaches, gastrointestinal problems, increased aggression, insomnia, anxiety, sexual dysfunction.
o Serotonin is released from platelets (vasoconstriction).

65
Q

Venlafaxine

Duloxetine

A

Type: Anxiolytics

Class: SNRIs

• Like TCAs: block monoamine re-uptake BUT they have no affinity for other targets (responsible for adverse effects)

66
Q

Propranolol

A

Type: Anxiolytics

Class: Beta-Adrenoceptor Antagonists

Reduce action of sympathetic system to allow sleep

Medicine (6 decks)

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