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Year 2 semester 2 > Drugs > Flashcards

Drugs Flashcards

1
Q

Interferons

A

Decreases proinflammatory cytokines
Increases antinflammatory cytokines
Inhibits entry of immune cells into the CNS
Interferes with T-cell adhesion to endothelium
Reduces T-cell activation by interfering with HLA class II molecules

Flu-like symptoms
Rash/necrosis at the site of injection
Cognitive changes e.g depression
Bone marrow failure

MS 1st line

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2
Q

Glatiramer acetate

A

Decoy protein for myelin basic protein

Flushing 
Rash
Chest tightness
Palpitation
Anxiety
Dyspnoea

MS 1st line (but after Interferons)

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3
Q

Natalizumab

A

Binds to alpha-4 integrins on CD52 T cells
Stops them binding to BBB

Hypersensitivity reaction, Develop neutralizing antibodies
MS 2nd line

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4
Q

Finglomod

A

Prevents progress of lypmhocytes from secondary lymphoid tissue

Slight Immunosuppression
MS 2nd Line

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5
Q

Mitoxantrone

A

Type II topoisomerase inhibitor
Prevents DNA transcription to RNA

Cardiotoxic
Max use 2-3 years
MS 3rd line

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6
Q

Methotrexate

A

Folate inhibitor
Immunosuppressant
MS 3rd line

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7
Q

Azathioprine

A

Purine analogue

Immunosuppressant

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8
Q

Glucocorticoids- methylprednisolone

A

Has anti-inflammatory and immunosuppressant effects. Affects both early and late stage inflammation. Decreases extravasation activation of neutrophils. Either: Upregulates expression of anti-inflammatory proteins in the nucleus or Represses the expression of proinflammatory in the cytosol.

Opportunistic infections
Sudden withdrawal can cause adrenal insufficiency, Cushing’s, osteoporosis, hyperglycaemia, depression and psychosis

MS Acute relapses

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9
Q

Analgesics: Paracetamol

A

Antipyretic , Weak COX inhibitor

1st line treatment for generalised headache

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10
Q

NSAIDS

A

COX inhibitors

Gastric problems

1st line treatment for generalised headache

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11
Q

Serotonin Agonists- Tryptans

A

Serotonin agonist
Block pain pathway
Inhibit vasoactive peptide release

Drowsiness

Severe Migraine 1st line

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12
Q

Serotonin Agonists- Ergots

A

Serotonin agonist

Worsening of nausea and vomiting
Rebound headaches

Severe migraine 2nd line

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13
Q

Beta adrenergic blocker: Propanolol

A

Beta adrenergic blocker

Bradycardia, Hypotension

Migraine prophylaxis

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14
Q

L-dopa: Levadopa

A

Dopamine precursor

Nausea/Vomiting
Hypertension
Psychosis
Long-term – Dyskinesia
Death

1st line PD, Usually given with COMT or decarboxylase

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15
Q

Dopamine receptor agonist: Bromocriptine (ergot)

A

Direct D2 agonist

Nausea
Postural hypertension
Sleep attacks (narcolepsy)
Chest and pulmonary problems

1st line PD, Not available on the PBS

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16
Q

Dopamine receptor agonist: Pramiprexol (non-ergot)

A

Direct D2-3 agonist

Nausea
Postural hypertension Sleep attacks narcolepsy)

Better tolerated than Bromocriptine

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17
Q

Monoamine oxidase inhibitor: Selegiline

A

Protects DA from degradation

Confusion
Delirium
Hypertension

2nd line PD, 4th line depression

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18
Q

Enzyme inhibitor: Decarboxylase inhibitor: Carbidopa

A

Protects L-dopa from degradation to dopamine in the peripheries

Confusion
Delirium

Adjunct 1st line for PD

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19
Q

Enzyme inhibitor: COMT

A

Reduces metabolism of L-dopa to 3-OMD Confusion , Delirium

Adjunct 1st line PD

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20
Q

Anticholinergenics: Benztropine, Benzhexone

A

Muscarinic receptor antagonist

Dry mouth
Nausea
Constipation
Palpitations
Arrhythmias

PD, Limited use for patients on antipsychotics

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21
Q

Antiviral: Amantadine

A

Increased release, inhibit reuptake, dopamine agonist , NMDA receptor antagonist

Less severe but similar to L-dopa

PD 2nd line (1st line for mild-moderate)

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22
Q

VMAT 2 Inhibitor: Terabenazine

A

Blocks DA transport into vesicles in presynaptic terminal, Depletes DA , Decreases dopamine transmission

Allergic reaction
Extreme drowsiness
Mood or behaviour changes 
Agitation
Tremor
Trouble swallowing
Dizziness or fainting

HD 1st line

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23
Q

Neruoleptics: Haloperidol, Risperidone, Olanzapine

A

HD 1st line (refer to antipsychotics)

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24
Q

GABA agonists: Baclofen

A

G-coupled receptor

Loss of muscle tone

HD 1st line

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25
Q

GABA Agonist: Clonazepam

A

Ionotropic receptor

Tolerance
Sedation
Coma

HD 1st line

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26
Q

Na+ channel blockers: Phenytoin, Carbamazapine, Lamotrigine, Primidone

A 
Acts on sodium voltage gated channels
Use dependent (Preferentially blocks neurons with higher activity)

Acne
Teratogenic
Hirsuitism
Hormone imbalances

Epilepsy
Focal seizures – 1st line Carbamazapine
Acute bipolar (mania)
Grand Mal – lamotrogine

27
Q

Ca2+ channel blockers: Ethosuxamide

A

T-type calcium channel blockers

GIT
Lethargy
Nausea/Vomiting

Absent seizures

28
Q

Valproate

A

Decreases rate of slow sodium channels
Decreased activity of t-type calcium channels
Decreases GABA transaminase
Increased GABA synthesis

GIT 
Fatigue
Hair loss
 Tremor
Rash

1st line most seizures and Acute bipolar (mania)

29
Q

Gabapentin

A

Sodium, calcium and GABA release

Somnolence
Dizziness

3rd line epilepsy

30
Q

Topiramate

A

AMPA receptor on glutamate, sodium and Calcium

Loss of cognitive function
Dizziness
Amnesia

3rd line epilepsy

31
Q

GABA Potentiator: Vigobatrin

A

Inhibits transaminase

Sedation
Drowsiness
Agression
Psychosis (rarely)

2nd line epilepsy

32
Q

GABA Potentiator: Benzodiazapines (Lorazepam, Diazepam, Clonazepam)

A

Increases frequency of CL channel opening

Sedation
Drowsiness
Muscle relaxant
Hypnotic

2nd line epilepsy, Anxiolytic 1st line acute panic attacks

33
Q

GABA potentiator: Midazolam

A

Increases duration of Cl channel opening

Sedation
Drowsiness

2nd line epilepsy

34
Q

GABA Potentiator: Barbituates (Phenobarbitol)

A

GABA-A cl- channel agonist, Increases duration of cl- opening

Sedation
Drowsiness

3rd line epilepsy

35
Q

GABA Analogue: Acamprosate

A

Increases GABA, NMDA receptor inhibition

Headaches
Diarrhoea
Pruritis (sometimes)

Protracted withdrawal (not recommended for acute phase)

36
Q

Enzyme blocker: Disulfiram

A

Blocks acetaldehyde dehydrogenase

Hangovers
Depression and psychotic symptoms
Peripheral neuropathy
Liver damage

Adjunct for alcoholism

37
Q

Opioid receptor antagonist: Naltrexone

A

Blocks (mu) opioid receptors

Prominent nausea
Headaches
Dysphoria

1st line for alcoholism withdrawal

38
Q

Monoamine inhibitors: Moclobemide, Selegiline

A

Inhibit MAO outside the mitochondria in the synaptic terminal

Significant hypertension when combined with tyramine
Tremors
Insomnia
Convulsions
Weight gain

4th line for depression

39
Q

Monoamine uptake inhibitors: SSRI (Sertraline Fluoxetine Paroxetine Citalopram Escitalopram)

A

Increase extracellular level of serotonin by inhibiting SERT

Headaches
Dizziness
Nausea
Hyponatremia
Serotonin Syndrome

1st line depression
1st line pharmacological treatment for GAD, panic attacks, eating disorders, OCD

40
Q

TCAs (Amitryptaline (tertiary amine)

Nortryptaline (secondary amine)

A

Inhibit reuptake of SERT and NET

Anti-cholinergic
Anti-histaminergic
Anti-adrenergic

3rd line for depression

41
Q

SNRIs (Venlaxafine, Desvenlaxafine)

A

Inhibit 5HT and NA reuptake
SSRIs plus CV risk
2nd line for depression

42
Q

NRI Reboxetine

A

Selective NET

Less SSRI types but increase CV effects
Insomnia

2nd line for depression

43
Q

Atypical tetracyclics: Mianserin

A

Increases NA release by blocking alpha2 adrenoreceptors (autoreceptors), Inhibits uptake of NA

Headache
Drowsiness
Fatigue
Dry mouth

44
Q

Atypical tetracyclics: Mirtazapine

A

Increases 5HT, NA release by blocking alpha2 adrenoreceptors and 5ht2 and 3 (autoreceptors)

Headache
Drowsiness
Fatigue
Dry mouth

45
Q

Mood stabiliser: Lithium

A

Targets secondary messenger systems that modulate neurotransmitters
Reduced excitatory eg. DA and Glut.
Increases inhibitory eg. GABA

Restlessness/tremors
Bloating
Fluctuations of weight
Acne
Alopecia
Depression

1st line therapy bipolar disorder

46
Q

Antipsychotics: Typical (Chlorpromazine, Haliperidol)

A

Strong antagonists of D2 and some D1
Weak antagonists at 5HT2 receptors
Main effects against positive symptoms

Dystonia
Parkinsonism
Hyperprolactemia
Akithesia
Tardive dyskinesia

2nd line for psychosis

47
Q

Antipsychotics: Atypical (Respiridone, Clozapine, Olanzapine, Reserpine)

A

Weak D2 antagonists, Strong 5HT2 antagonists
Efficacy against positive and negative symptoms

Weight gain
Agranulocytosis
CVS risk

1st line for:
Acute and chronic psychosis
Acute mania
Organic psychosis
Severe behavioural disorders in children
Tourette’s
Other choreas
48
Q

Thyoid Hormone replacement: Levothyroxine

A

Acts as a T4 analogue which is partially converted to T3

Cardiovascular – palpitations, tachycardia, arrhythmias angina, cardiac arrest
CNS – tremors, headache, nervousness insomnia, GI – diarrhoea, vomiting, Hypersensitvity, Weight loss, Menstrual irregularities, Sweating, Heat intolerance

Treatment of choice in hypothyroidism

49
Q

Beta Blockers: Propranolol

A

Relieves tachycardia, tremor, diaphoresis, anxiety No effect on underlying hormone secretion

Used for symptomatic relief until hypothyroidism is resolved

50
Q

Thioureas: Carbimazole and Propylthiouracil

A

Inhibits thyroid synthesis by concentrating in the thyroid gland and inhibiting the organic binding of I2. Inhibits iodination of tyrosine residues.

Headache
Joint pain
Rashes
Pruritis
GIT disturbances
Alopecia
Jaundice
Myopathies
Abnormal blood cells
Agranulocytosis (within 60 days)	Hyperthyroidism

Hyperthyroidism 1st line , Adjunct to radioactive iodine

51
Q

Radiotherapy: Radioactive Iodine (131)

A

Taken up and processed the same was as normal iodine. Emits beta and gamma rays. The beta particles are absorbed by the tissue and has a powerful cytotoxic effect. This effect is restricted to thyroid follicle cells

Hypothyroidism

1st line for hyperthyroidism

52
Q

Insulin Sensitiser: Biguanides Metformin

A

Reduce hepatic glucose output through activation of enzyme of AMP activated protein kinase
Increase glucose uptake by peripheries
Mechanisms are unknown

Nausea
Vomiting
Abdominal discomfort
Diarrhoea
Weight loss

1st line Diabetes type 2

53
Q

Insulin sensitiser: Glitazones, Pioglitazone, rosiglitazone

A

Ligands of peroxisome proliferator activated receptor gamma (PPAR-g). Modulate expression of genes involved in lipid and glucose metabolism, insulin signal transduction, tissue differentiation. Increased lipogenesis

Fluid retention
Immune system
Increased risk of heart failure
Loss of bone mineral density
Weight gain

3rd line Diabetes type 2. With continued metformin and insulin secretagogues

54
Q

Insulin secretagogues: Sulfonylureas

A

Binds to ATP-sensitive potassium channels on the surface of pancreatic B-cells. Closure of the channel and depolarisation of the B cell Ca entry
Insulin release

Hypoglycaemia

1st line Diabetes Type 2, Only used in patients with some beta cell function

55
Q

Insulin secretagogues: Meglitinides, repaglitinide

A

Modulate beta-cell insulin release by regulating potassium efflux through the same potassium channels as sulfonylureas

Hypoglycaemia, Weight gain

Greater effect on post-prandial increases in blood glucose than on fasting

56
Q

Alpha glucosidase inhibitors: Acarbose, miglitol

A

Competitive inhibitor of alpha-glucosidase
Mimimize upper intestinal digestion and defer digestion of the ingested starch

2nd line Diabetes type two
With metformin and insulin secretagogue

57
Q

Incretin enhancers

A

Inhibit the activity of dipeptidyl dipeptidase the enzyme that main enzyme that break downs GLP-1 and GIP. This inhibits secretion of the glucagon and inhibits gastric emptying and thus delays glucose absorption

Headache
Nausea
Diarrhoea
Increased rate of infections

2nd line Diabetes type 2
With metformin and insulin secretagogue

58
Q

Amylin analogues: pramlitine

A

Supresses glucagon release
Delays gastric emptying

Adjuncts diabetes treatment

59
Q

Adrenal enzyme inhibitors: Ketoconazole and aminoglutethimide

A

Inhibits cytochrome p450 enzymes P450scc and P450c11

Adjunctive therapy while in patients with mild disease while waiting for pituitary irradiation works

60
Q

Adrenal steroidgenesis blockers: Metyrapone

A

Control hypersecretion of cortisol

Adjunct therapy in treatment of Cushing’s syndrome

61
Q

Adrenolytic: Mitotane

A

Adrenal atrophy predominantly in zona fasciculate and reticularis

Severe nauseas
Vomiting
Diarrhoea
Skin rashes

62
Q

Adrenal replacement therapy: Corticosteriods (hydrocortisone)

A

Acts to replace cortisol

63
Q

Mineralocorticoid supplements: fludrocortisones

A

Acts to replace aldosterone

64
Q

Biphosphonates: Alendronate, risedronate

A

Inhibit osteoclast induced bone resorption, Increase bone density, Reduce incidence of fractures

Nausea
Chest pain
Hoarseness

Osteoporosis

Year 2 semester 2 (10 decks)

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