B+B Drugs

Front 1

PARKINSONS drugs:

Back 1

Front 2

PARKINSONS drugs:

what optimises the effect of L-DOPA?

Back 2

Entacapone (a COMT inhibitor)

Front 3

What are the adverse effects of L-DOPA?

Back 3

Nausea, vomiting

Postural hypotension

Psychosis

Impulse-control disorders

Excessive day-time sleepiness

MOTOR:

on-off effect

wearing off effect

dyskinesia and dystonia

Front 4

PARKINSONS drugs: what drugs are given at an early stage?

Back 4

Beign MOA-B inhibitor.

Front 5

PARKINSONS drugs: what drugs are given for mild-moderate disability without cognitive impairment?

Back 5

Dopamine agonist

Front 6

PARKINSONS drugs: what drugs are given for moderate to severe impairment?

Back 6

Levodopa with a COMTI

Front 7

PARKINSONS drugs: What are non-drug treatment options?

Back 7

Human embyronic mesencephalic graft

Stimulation: of the sub thalamic nucleus

Pallidotomy

Front 8

HUNTInGTON's drugs

Back 8

Palliative and symptomatic:

Antidopaminergic (= aytpical antipsychotic drugs) = tetrabenazine, haloperidol, olanzapine

Antidepressant drugs = imipramine

amityptiline.

Front 9

DBS: what are the potential uses?

Back 9

Implant into STN in Parkinson's disease

Tourette Syndrome

Major Depressive disorder

Obsessive compulsive disorder.

Front 10

Outline the mechanism of DBS:

Back 10

Application of mild, adjustable and reversible electrical current to target sites.

Stimulation causes pattern changes across populations of neurones resulting in modulation.

Suppress abnormal oscillations in basal ganglia networks.

Stimulation results in the activation of outputs. this results in a change in neuronal activity.

Front 11

STROKE treatment:

Back 11

1. Thrombolysis if infarct: tpA

2. Transfer to stroke unit

3. Antiplatelet therapy = 300mg aspirin and then 75mg clopidogrel

4. Address risk factors

5. Treat complications

6. MDT rehabilitation

7. Advice and education

Front 12

MS Treatment: What are the top 3 drugs?

Back 12

Natalizumab

Alemtuzumab

Fingolimod

Front 13

What are other MS drugs?

Back 13

IFN Beta/GA

Teriflucomide

DMF

Phase 3 trials: ocrelizumab, daclizumab, laquuinimod.

Phase 2 trials: simponimod, firategrast, ofatumumab.

Front 14

What is the aim in MS treatment?

Back 14

NEDA = no evidence of disease activity = no relapses, no sustained disability progression, no MRI activity.

Front 15

Name 3 orally-adminisited MS drugs:

Back 15

Teriflunomide

Fingolimod

DMF

Front 16

How are Natalizumab and Alemtuumab administered?

Back 16

IV

Front 17

PAIN: centrally acting analgesics: What are the key forms?

Back 17

1. Opiates: morphine, codeine, heroin = are all agonists for mu opioid receptors that bind endogenous enkepahlin found on lamina 1 cells and C fibre afferents.

Block the excitatory action of the C fibres on lamina 1 cells.

2. Clondine, an Alpha 2 adrenoceptor agonist - has effects similar to GABA-ergic interneurons. (presynaptically inhibit the primary afferent and postsynaptic inhibition of the projection neurone- inhibitory)

Front 18

PAIN: how does acupuncture work?

Back 18

Thought to activate A delta fibres and in doing so descending inhibitory control of nociception.

Analgesia can also be produced by stimulation of non-noxious afferents.

Stimulate lamina 2 cells.

Basis of TENS.

Front 19

Depression/Anxiety: what are the aspect to CBT?

Back 19

Front 20

PAIN: describe the mechanism of action of morphine:

Back 20

Activates K+ conductance out of the cell and decreases calcium conductance into the cell.

OVERALL - decreases the excitability and decreases the release of neurotransmitters.

Front 21

PAIN: name 3 opioids:

Back 21

Morphine

Codeine

Tramadol

Front 22

PAIN: what are some of the negative S/Es of opioids?

Back 22

CNS: analgesia, resp depression, drowsiness, euphoria or dysphoria, miosis, nausea and vomitting.

CVS: hypotension

GI system: delayed gastric emptying and decreased biliary and pancreatic secretions

Urinary urgency

Itching

Front 23

PAIN: what is the metabolite of morphine that can aciculate if renal function is impaired?

Back 23

M6G metabolite.

Front 24

PAIN: outline the opioid ladder:

Back 24

Front 25

PAIN: non-opioids: what is the mechanism of action of Paracetamol?

Back 25

It reduces the active oxidised form of COX-2 and modulate the endogenous cannabinoid system.

Analgesic, antipyretic but little anti-inflammatory effect.

Front 26

PAIN: non-opioids: what is the mechanism of action of NSAIDs?

Back 26

They inhibit COX enzymes:

Aspirin: COX1 and COX2 inhibitors: analgesic, antipyretic, anti-inflam. (prevent prostaglandin formation)

Ibuprofen, diclofenac and ketoprofen: also inhibit COX-1 and COX-2 inhibition. Plus additional mechanisms…analgesic and anti-inflammatory effects.

Front 27

PAIN: name a selective COX-2 inhibitor:

Back 27

Refecoxib.

Front 28

PAIN: what are the indications and side effects of NSAIDs?

Back 28

Indicated for: rheumatoid arthritis, osteoarthritis, dysmenorrhea, gout and muscle spasm.

SEs: nausea, GI bleeds.

Front 29

PAIN: non-opioids: name and explain the MOA of anticonvulsant drugs:

Back 29

1. Carbamazepine: acts on sodium channels.

2. Sodium valproate: acts on sodium channels.

3. Pregabalin: acts on the alpha 2 delta sub unity of calcium channels.

Front 30

What are the indications for antidepressants and what is the MOA?

Back 30

Neuropathic pain, cancer, depression, Huntington's disease.

TCADs inhibit the reuptake of amines and also block sodium and calcium channels.

Front 31

PAIN: What medication are used for migraines?

Back 31

Triptans

Ergoatamine derivatives

Front 32

PAIN: State the key receptors involved in complex types of pain:

Back 32

Front 33

PAIN: what are the 1st, 2nd and 3rd line drugs for neuropathic pain?

Back 33

1st line - SNARIs = duloxetine and venlafaxine

TCAs

Pregabalin, gabapentin (calcium channel ligands)

2nd line -

Tramadol

Capsaicin patches (vanilloid receptors)

Lidocaine

3rd line-

Strong opioids

Botulinum toxin A

Front 34

PAIN: name 3 local anaesthetics and their MOA.

What is the main risk?

Back 34

Lignoicaine, bupivacaine, prilocaine

MOA: blockage od sodium channels.

Risks: systemic toxicity, hypotension, resp depression and bradycardia.

Front 35

PAIN: what is the modes of administration and MOA of general anaesthetics + their major risk:

Back 35

Inhaled or IV

MOA: activation of inhibitory receptors or inhibition of excitatory receptors

RISK = induce CV depression

Front 36

PAIN: Name 4 Inhaled and 4 IV general anaesthetics:

Back 36

Inhaled:

Halothane

Enflurane

Isofulrane

Nitrous oxide

IV

Propofol

Thiopental

Etomidate

Ketamine

Front 37

PAIN: how is trigeminal neuralgia treated?

Back 37

Carbamazepine

Baclofen

Phenytoin

Valproate

Clonazepam

Front 38

EPILEPSY: anti epileptic drugs: what are the main classes?

Back 38

Sodium channels

Benzodiazepines

Barbiturates

Calcium channels

Neurotransmitter uptake

Neurotransmitter release

Neurotransmitter synthesis

Neurotransmitter receptors

Front 39

EPILEPSY: anti-epileptic drugs:

Back 39

Front 40

EPILEPSY: explain the meaning of zero order or saturation kinetics of Phenytoin:

Back 40

Front 41

EPILEPSY: what drugs act on sodium channels?

Back 41

Front 42

EPILEPSY: what drugs act on calcium channels?

Back 42

Front 43

EPILEPSY: what drugs are GABA A receptor positive allosteric modulators?

Back 43

Front 44

EPILEPSY: what drugs act on:

NT release?

NT uptake?

NT synthesis?

Back 44

Front 45

EPILEPSY: what do Vigabatrin and Tiagabine inhibit?

Back 45

Relevant because epilsepy may be accompanied by a loss of cortical chandelier GABA-ergic cells.

Front 46

EPILEPSY: what drugs should be given for each type of epilepsy?

Back 46

Front 47

EPILEPSY: how should status epileptics be managed?

Back 47

It is a medical emergency. Treat with Diazepam IV.

May be potential for vagal nerve stimulate and DBS in the future.

Front 48

ADDICTION: what are the broad classes of treatments?

Back 48

Front 49

MS: name some key anti-spastic drugs that are currently used in MS

Back 49

Front 50

CANNABINOIDS: what is Rimonabant?

Back 50

CB1 Antagonist

Anti-obesity drug

Front 51

DRUG DEPENDANCE: classify drugs of abuse into CLass A, B and C:

Back 51

Front 52

DRUG DEPENDANCE: what are the key receptors for drugs of abuse?

Back 52

Front 53

DRUG DEPENDANCE: what is ecstasy?

Back 53

Front 54

DRUG DEPENDANCE: what are the MDMA targets?

Back 54

Front 55

DRUG DEPENDANCE: what are the symptoms of acute MDMA toxicity?

Back 55

Front 56

DRUG DEPENDANCE: what are the risks of smoking cannabis?

Back 56

Front 57

DRUG DEPENDANCE: name a CB1 receptor agonist that is used therapeutically:

Back 57

Front 58

DRUG DEPENDANCE: how can nicotine addiction be managed?

Back 58

Nicotine replacement therapy- nicotine agonists

Bupropion - monomamine- especially dopamine reuptake inhibitors.

Front 59

DRUG DEPENDANCE: how can opiate addiction be managed?

Back 59

Methadone = opioid agonist

Buprenorphine - mu receptor, partial agonist, kappa antagonists

Clonidine and lofexidine - alpha 2 adrenreceptor agonists

Naltrexone: relapse prevention.

Front 60

DRUG DEPENDANCE: what is Varenicline?

Back 60

Varenicline: is a

α4β2 partial agonist

Adverse effects: nausea, psychiatric disturbances (FDA black box warning)

Front 61

DRUG DEPENDANCE: how can cocaine/crack addiction be managed?

Back 61

Detoxification and anti-cocaine vaccine

Front 62

DRUG DEPENDANCE: how can alcohol addiction be managed?

Back 62

Front 63

DEPRESSION: TCADS:

Back 63

Front 64

DEPRESSION: SSRIS

Back 64

Front 65

DEPRESSION: MAOIS

Back 65

Front 66

DEPRESSION: Explain the delay of action of TCADs:

Back 66

•Tricyclic drugs inhibit reuptake of amines

•The immediate increase in synaptic concentration of amines

may lead to activation of somatic neuronal autoreceptors (e.g. 5-HT1A type)

•The activated autoreceptors decrease firing of the neurones

•During the first weeks of treatment the autoreceptors desensitize

•The neurones will return subsequently to the normal firing rate

•The inhibition of reuptake continues and the level of amines continues to be high

Front 67

DEPPRESION: what is escitalopram?

Back 67

It is a new S-isomer of citalopram

Front 68

DEPRESSION: Reversible MAOIs:

Back 68

Front 69

DEPRESSION: what/where does Venlafaxine and Reboxetine act?

Back 69

Front 70

DEPRESSION: What is Agomelatine?

Back 70

Recent drug with new mechanism of action: agonist at melatonin MT1

and MT2 receptors and antagonist at 5-HT2c receptors

(may act as a noradrenaline/dopamine disinhibitor)

Onset of effect in the first week of treatment; improves sleep quality;

less sexual dysfunction than SSRIs; anxiolytic effects; no discontinuation

syndrome

Front 71

BIPOLAR: how can Bipolar be managed?

Back 71

Lithium: used as maintenance treatment in bipolar disorder, acute mania and drug-resistant depression

Narrow therapeutic margin (0.6-1mM)

Renal and thyroid function checked before treatment (and then at regular intervals during maintenance treatment)

Adverse effects: thirst, nausea, fine tremor, polyuria, weight gain, oedema, acne

Front 72

MOOD STABILISERS: state two mood stabilising drugs that are also used in epilepsy and for neuropathic pain:

Back 72

Front 73

MOOD DISORDERS: what are the non-pharmacological approaches?

Back 73

Front 74

SCHIZOPHRENIA: what are the typical antipsychoitcs used?

Back 74

Typical antipsychotics (neuroleptics)

chlorpromazine, thioridazine,

fluphenazine, haloperidol, flupenthixol

Front 75

SCHIZOPHRENIA: what are the atypical antipsychoitcs used?

Back 75

Atypical antipsychotics (neuroleptics)

risperidone, olanzapine, clozapine, quetiapine

•Atypical neuroleptics may improve cognition (MODERATE EFFECTS)

•All atypicals also have significant antagonist activity at 5-HT2 receptors

•Clozapine blocks D4 receptors with high affinity

Front 76

SCHIZOPHRENIA: what are adverse effects of using antipsychoitcs used?

Back 76

Extrapyramidal effects (acute dystonias, parkinsonism,

tardive dyskinesia)

Rise in prolactin (galactorrhoea, amenorrhoea)

Weight gain (atypicals)

Dyslipidemia (atypicals)

Type 2 diabetes (atypicals)

General - allergic and toxic reactions,

Anticholinergic effects (clozapine, haloperidol)

Postural hypotension

Front 77

SCHIZOPHRENIA: name a rare antipsychotic drug complication:

Back 77

Neuroleptic malignant syndrome

• hyperpyrexia

• rigidity

• confusion

• autonomic instability

Front 78

SCHIZOPHRENIA: what is an irreversible complication of antipsychotics?

Back 78

Tardive Dyskinesia.

Front 79

SCHIZOPHRENIA: what is Clozapine?

Back 79

It is the drug of choice in drug resistance.

but risk of aggranulocytosis.

Front 80

SCHIZOPHRENIA: name two drugs that can be given as depot injections:

Back 80

Fluphenazine, Haloperidol.

Front 81

ANXIETY: what are the main classes of anxiolytics?

Back 81

•Benzodiazepines (clonazepam, alprazolam…) = positive allosteric modulators of the GABA A receptor complex.

•5-HT1A agonists (buspirone, ipsapirone) partial agonism

•β-antagonists (propranolol…)

•SSRIs (fluoxetine, escitalopram, paroxetine…)

•Barbiturates (obsolete)

Front 82

ANXIETY: how do benzodiazepine and barbiturates effect the GABA A channel?

Back 82

Front 83

ANXIETY: how can benzodiazepine overdose be managed?

Back 83

With Flumaxenil.

Front 84

ANXIETY: what are the treatments for Generalised Anxiety disorder?

Back 84

buspirone

•venlafaxine, duloxetine (SNRI)

•fluoxetine, escitalopram (SSRI)

•risperidone, quetiapine, olanzapine (APD)

Front 85

ANXIETY: HYPNOTICS: what are the unwanted effects of benzodiazepines used as hypnotics?

Back 85

Unwanted effects of benzodiazepines used as hypnotics

•Change in sleep patterns (suppress deep sleep and REM sleep)

•Daytime sedation

•Rebound insomnia

•Tolerance

•Dependence (withdrawal syndrome characterised by anxiety, nausea, muscle cramps, seizures)

Front 86

ANXIETY: what are the complications of benzodiazepines in the elderly?

Back 86

Psychomotor impairment

Risk of falls

Daytime drowsiness

Intoxication

Amnesia

Depression

Respiratory problems

Abuse and dependence

Front 87

DEMENTIA: what are the 2 classes of drugs used as treatment?

Back 87

Front 88

DEMENTIA: what is the MOA and side effects of using MEMANTINE?

Back 88

Front 89

DEMENTIA: what symptomatic medication may be used?

Back 89

Front 90

DEMENTIA: what are some potential disease modifying therapies?

Back 90