Pharmocology Flashcards

1
Q

Proton Pump Inhibitors:

What do the names of the drugs end in?
What is a prodrug?
What is their protective coating made from?
What cells are they taken up by?
What do they form in the blood?
Why do they last a few days?
A
Name: ‘zole’
Prodrug: Enters inactive 
Protective coating: H2CO3- to alter pH
Uptake: Parietal cells
Form: Suldenamides in the blood
Long lasting: Irreversibly bind
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2
Q

Histamine (H2) Antagonists:

What is the normal action of Histamine?
What do H2 antagonists do?
What do the names of the drugs end in?

A

Action: Binds to H2 receptor –> G protein –> adenylate cyclase –> cAMP –> Protein kinase A –> protein phosphorylation and activation –> increases acid
Antagonists block this
Name: ‘tidine’

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3
Q

NSAIDS’s:

What is the normal action of the COX1 enzyme?
What is the normal action of the COX2 enzyme?
What do NSAID’s do?

A

COX1: Prostaglandin increase mucus and decrease acid in the stomach
COX 2: Cause inflammation due to illness
Drugs: Stop the inflammation but also decrease mucus and increase acid in the stomach

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4
Q

Misoprostal:

What molecule is it a similar shape to?
What does it do in the stomach?

A

Similar shape to prostaglandin

Maintains mucus

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5
Q

Muscarinic antagonists:

What do they treat?
What do the names of the drugs end in?
Side effects?

A

Treat: Motion sickness
Name: ‘cine’
Side effects: Blurred vision, relaxed gut and dry mouth

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6
Q

Histamine (H1) Antagonists:

What do they treat?
What do the names of the drugs end in?
Side effects?

A

Treat: Motion and morning sickness
Name: ‘zine’
Side effects: Drowsiness and dry mouth

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7
Q

What drug which was used for morning sickness was banned and why?

A

Thalidomine

Developmental problems in the limbs

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8
Q

5HT3 antagonists:

How do they work?
How can you increase their effectiveness

A

Target 5HT stimulation

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9
Q

Other drugs for sickness:

Metaclopramide: How it works and side effects.
Phenothiazides: What do the drugs end in and side effects
Doperidone: What does it act on and what can it not cross?

A

Metaclopramide:
Acts on the chemoreceptor trigger zone and increases digestive motility.
Side effects: movement+menstruation disorders, fatigue, increased prolactin

Phenothazides:
‘zine’ and neurological effects

Doperidone:
Acts on chemoreceptor trigger zone and the gut
Cannot cross the blood brain barrier

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10
Q

2 interventions for autoimmune disease

What do these drugs do?
Rituximab
Atabercept
Ipilumumab

A

Cytokine therapies block the problematic antibody (e.g. anti-TNF/anti-IL1)
Steroids to stop clonal expansion by blocking receptors and signal recognition

Rituximab: Anti B cell antibodies
Atabercept: Inhibits T cell response by blocking positive signals
Ipilumumab: Stimulates antibody causing positive signal and decreased T cell activity

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11
Q

Name 2 anti-platelet drugs

A

Aspirin and Clopidogrel

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12
Q

What 2 things does Aspirin do in the vasculature?

3 uses and one problem

A

Inhibits COX 1 which is used to activate thromboxane A2
Inhibits COX2 in vasculature endothelial cells causing decreased inflammation
Uses: Angina, heart attacks, stroke (can also cause stroke)

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13
Q

What type of drug is Clopidogrel?
What does it do?
How is it metabolised?
Side effect?

A
Clopidogrel:
An ADP receptor antagonis
Inhibits ADP (a platelet agonist released from dense granules)
Metabolised by P450 enzymes 
Side effects: Bleeding
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14
Q

What do anti-coagulants do?
What are the 2 types?
Name 2 anti-coagulant drugs

A

Decrease the formation of fibrin by inhibiting the synthesis/activity of clotting factors

Direct thrombin inhibitors / direct factor 10 inhibitors

Heparin and Warfarin

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15
Q

What are the two types of Heparin and how are they made?

What are the differences between them?

A

Unfractionated Heparin is a natural polysaccharide which can be fractionated to LMW Heparin

UFH binds to antithrombin and inactivates factor 10 and thrombin by forming a ternary complex
LMWH only inactivates factor 10 as it does not form this complex

Side effects: Immune induced thrombocytopenia, neurological injury

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16
Q

What clotting factors rely on the reduced form of Vitamin K?

Use and side effects of Warfarin?

A

7,9,10
Use: Prevents clotting after heart attacks
Side effects: Osteoporosis, bleeding, foetal haemorrhage

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17
Q

How does high levels of Aspirin increase the risk of a myocardial infarction?

A

COX 2 produces prostacyclin which switches platelets off and vasodilates; when this is blocked platelets are switched on and the vessels are vasoconstricted –> clots

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18
Q

How does Aspirin actually work?

A

Stops platelets from metabolising arachidonate acid to thromboxanes
Arachidonate acid is therefore metabolised to lipoxins which solve the response

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19
Q

What are ‘coxibs’

Example

A

COX 2 specific drugs

Celecoxib

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20
Q

4 side effects when Coxibs and ibuprofen are taken together

A

Hyponatraemia
Heohrotoxicity
Bleeding
Hyperkalaemia

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21
Q

What does ‘NO-NSAID’ stand for?

2 positive effects?

A

Nitric oxide-donating NSAID

Gastric protection and increased anti inflammatory effects

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22
Q

4 roles of Glucocorticoids

3 example drugs

A

Decrease inflammation caused by cytokines
Decrease prostaglandins and leukotrines
Decrease emigration of leukocytes from vessels
Increase apoptosis of lymphocytes and eosinophils

Hydrocortisone, Prednisolone, Dexamethasone

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23
Q

What are the three levels of steroid dose?

How is toxicity affected by these levels?

A

Topical: Low dose
Acute: Medium dose
Chronic: High dose

Higher dose = higher toxicity

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24
Q

Side effects of steroids (4)

A

Decreased response to infection
Decrease in steroid production
Carbohydrate and protein metabolism effects
Cushing’s syndrome

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25
Q

What do glucocorticoids inhibit?

Why does this lead to such a large effect?

A

Inhibit phospholipase A

Whole cascade is disrupted

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26
Q

2 examples of sedating antihistamines
2 examples of non-sedating antihistamines
How are non-sedating antihistamines different?

A

Chlorphenamine and Promethazine
Cetrizine and Fexofenadine
They decrease vascular permeability

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27
Q

What is the mechanism of Basilximab?

A

Pick up cytokine in blood and prevent it from binding OR bind to the receptor and prevent the cytokine from binding
Prevent proliferation by blocking JAK signalling

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28
Q

What is the mechanism of Cyclosporine and Tarcolimus?

A

Both bind to different primary molecules but then go on to block the same protein which is needed for dephosphorylation of a compound which activates IL2 transcription in the nucleus

IL2 activates T cells so without dephosphorylation, T cells are not activates

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29
Q

What is the mechanism for Rapamycin?

A

Blocks the protein mTOR which activates protein synthesis, cytoskeleton activation and migration of immune cells
Also blocks proliferation as mTOR also activates cyclins that help G1–>S phase in the cell cycle

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30
Q

What are DMARDs

5 examples

A

Disease modifying anti-rheumatic drugs

Methotrexate, Gold, Sulfasalazine, Penillamide, Chloroalanine

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31
Q

What does the drug Carbamazepine do?

What 2 things does it treat?

A

Increases the inactivated state of the sodium channel and refractory period
Treats nerve pain and epilepsy

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32
Q

What does Tetrodotoxin do?

What does it cause?

A

Blocks Na ion channels

Respiratory depression

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33
Q

What do local anaesthetics do?

Give 2 examples of esters and 3 examples of amides

A

Block sodium ion channels

Esters: Cocaine and Procaine
Amides: Lidocaine, Bupiracaine, Ropivacaine

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34
Q

What are the 4 classes of opioids?

e.g. of each

A

Natural e.g. morphine
Endogenous e.g. endorphin
Semi-synthetic e.g. heroin
Fully synthetic e.g. pethidine

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35
Q

When should you not give opioids?

A

Alcoholism

Respiratory depression

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36
Q

What receptors do opioids bind to in the brain?

A

Mu, Delta, Kappa

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37
Q

Side effects of opioids?

A

Constipation, drowsiness, hypotension, nausea, respiratory depression and vomiting

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38
Q
What are the roles of these 7 opioids?
Morphine Sulphate 
Diamorphine (Heroin)
Codeine
Fentanyl
Pethidine
Tramadol
A

Morphine Sulphate: Most common
Diamorphine (Heroin): Increased power
Codeine: Mild-moderate relief, decreases cough and causes constipation
Fentanyl: Anaesthetic properties
Pethidine: Moderate-severe relief, obstetric and peri-operative
Tramadol: Decreases side effects by enhancing adrenergic and serotenergic pathways

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39
Q

What is the role of Naloxone?

A

An opioid receptor antagonist to reverse the effects of an opioid overdose

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40
Q

What drug is used to treat motor neurone disease?

What does it do?

A

Riluzole

Blocks glutamatergic neurotransmission to slow the progression of the disease

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41
Q

What is L-DOPA?

3 side effects?

A

Precursor of dopamine

Drug resistance, psychosis and involuntary movements

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42
Q

Side effect of a dopamine agonist?

A

Sleepiness

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43
Q

What is the treatment for Alzheimer’s - why?

3 examples of drugs

A

AChE inhibitors as there are decreased neurones in the hippocampus meaning ACh levels are reduced

Donepezil, Neostigmine, Physostigmine

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44
Q

What drugs do GABA receptors have binding sites for?

A

Benzodiazapines, Neurosteroids, Pricrotoxin, Barbiturates

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45
Q

What type of drug is Diazepam?

What does it do?

A

A anticolytic drug

Increases GABA inhibition–> hyperpolarisation

46
Q

How does the drug Picrotoxin work?

A

Stops the GABA ion channel from opening causing convulsion

47
Q

What does strychine poisoning cause?

A

Convulsion

48
Q

What do SSRI’s specifically inhibit?

What receptors do they inhibit and where are these receptors found?

A

SERT receptors

5-HT1A receptors in brain regions that control mood, cognition and theory

49
Q

4 examples of SSRI’s

A

Escitalopram
Fluoxetine
Busprione
Citalopram

50
Q

What neurotransmitters do MAO inhibitors affect?

A

Prevent serotonin and noradrenaline breakdown

51
Q

How do tricyclics work?

A

Block the uptake of serotonin and noradrenaline

52
Q

What drugs are used to treat chronic pain?

A

NSAID’s
Paracetamol
Opioids
Tricyclic Antidepressants

53
Q
What class of drugs are benzodiazepines?
What do they treat?
A

GABA-A agonists

Anxiety

54
Q

4 examples of Benzodiazepines

A

Diazepam, Temazepam, Colanezpam, Lorzepam

55
Q

8 side effects of Benzodiazepines

A

Addiction, amnesia, confusion, decreased coordination, drowsiness, sedation, muscle relaxation, withdrawal symptoms

56
Q

How do beta blockers help with anxiety?

A

Decrease the physical symptoms

57
Q

How do antipsychotic drugs work?

What symptoms do they treat?

A

Block D2 receptors in the MESOLIMBIC pathway

+ symptoms

58
Q

3 examples of antipsychotic drugs

Which are 1st and 2nd generation

A

1st generation: Haloperidol

2nd generation: Olanzapine and Risperidone

59
Q

Antipsychotic side effects on:

H1, Muscarinic, Alpha 1 adreno and 5HT2C receptors

A

H1: Sedation
Muscarinic: Dry mouth, blurred vision, decreased bowel and urine movements
Alpha 1 adreno: Postural hypotension
5HT2C: Increased appetite

60
Q

3 general side effects of antipschotic drugs

A

Cardiovascular and diabetes risk, cholesterol increase

61
Q

How do tricyclic antidepressants work?

3 things they treat

A

Block noradrenaline and serotonin reuptake transporters

Treat depression, pain and anxiety

62
Q

2 examples of tricyclic antideressants

A

Aminotryptiline and Lofepramin

63
Q

Side effects of SSRI’s

A

Nausea, suicide idealaition, sexual dyfunction and withdrawal

64
Q

Which is the safest anti-depressent to overdose on?

A

SSRI’s

65
Q

2 examples of MAO

A

Phenzine and Moclopemide

66
Q

Which antidepressant does not work on neurotransmitters?

A

Iprinidole

67
Q

What do beta blockers stop?

A

Tachycardia

68
Q

What is a side effect of a beta blocker?

A

Sweating

69
Q

What do botox and nerve gases block?

Where?

A

Both block cholinesterases

Botox in muscles and nerve gases in ganglia

70
Q

Give two examples of antidotes for sarin

A

Atropine and Pyridostigmine

71
Q

Give 4 examples of anaesthetics

A

Curare, Atacurium, Paniculonin and Miracurium

72
Q

What 2 things do nicotinic anaesthetics cause?

Give an example

A

Tonic paralysis and respiratory depression

Suxamethonium

73
Q

Is suxamethonium a long or short acting drug?

A

Short acting

74
Q

What is another name for hyosine

A

Scopolamine

75
Q

Give three examples of muscarinic antagonists

A

Tropicamide, Hyoscine and Atropine

76
Q

What type of drug is atropine?

What does it do?

A

A nicotinic and muscarinic antagonist

Nicotinic: Relaxes and dilates eye muscles
Muscarinic: Affects secretion, increases brachycardia, increases gut motility and decreases motion sickness

77
Q

What drug has similar effects as Atropine when it works as a muscarinic antagonist

A

Hyoscine

78
Q

Give an example of a muscarinc agonist

What does it do?

A

Pilocarpine

Iris constriction

79
Q

What two drugs stimulate the adrenergic neurone?

A

Caffeine and cocaine

80
Q

What class of drugs is Isoprenaline and Salbutamol?

A

Alpha antagonist and beta agonist

81
Q

Which is the more long term drug: Isoprenaline or Salbutamol?

A

Isoprenaline: ST as metabolised by CATACOLINOTRANSFERASE
Salbutamol: LT as inhibits this enzyme

82
Q

What do Isoprenaline and Salbutamol affect in the blood?

A

Blood pressure and peripheral resistance

83
Q

Give two examples of alpha antagonists

A

Phenoxybenzamine and Prazonin

84
Q

Give 2 examples of beta antagonists

Which one only works on beta 1?

A

Propanalol and Atenolol

Atenolol = beta 1 only

85
Q

Give 2 examples of beta 1 agonists

A

Dopamine and Dobutamine

86
Q

Give 3 examples of beta 2 agonists

A

Salbutamol, Terbutline and Salmeterol

87
Q

What does phenoxybenxamine work on?

A

Adrenal gland tumours that release noradrenaline and adrenaline

88
Q

What are the two classes of antipsychotic medications?

Which has more side effects?

A

1st and 2nd generation

1st generation has more side effects

89
Q

What class of drugs are antipsychotics?

A

D2 antagonists

90
Q

What neurotransmitters does Clozapine also affect aside from dopamine?

A

Noradrenaline and histamin

91
Q

Is Olanzapine sedative or not sedative?

A

Very sedative

92
Q

side effects of antipsychotics

A

20 year decrease in life expectancy, Breast enlargement, Cardiac issues, Diabetes, Q-T interval increases, Menstrual cycle changes, Milk leakage, Sedation, Sexual Dysfunction, Tachycardia, Weight increase

93
Q

One way that antipsychotics cause weight increase aside from by a natural increase in appetite

A

They increase histamine levels

94
Q

3 examples of immunosupressants which target transplantation

A

Cyclosporin, Tarcolimus, Sirolimus

95
Q

1 example of cytostatics for autoimmune disease

A

Cyclophosphamide

96
Q

1 example of cytotoxic (chemotherapy) agents for cancer

Explain how it works

A

Fluorouracil
Similar shape to T and U which leads to blocking
Inhibits enzymes causing apoptosis

97
Q

What drug is used to reduce cough?

A

AF-219

98
Q

What is the mechanism of action for the antibiotic Tetracycine?

A

Blocks tRNA entry to ribosomes

99
Q

What is the mechanism of action for the antibiotic Chlorampenicol?

A

Blocks new amino acids from entering the polypeptide chain

100
Q

What do aminoglycoside antibiotics target?

A

Ribosomes

101
Q

What do vaccinations target?

A

Capsules of bacteria

102
Q

What does penicillin target?

A

It disrupts the synthesis of the gram negative cell wall

103
Q

What do beta-lactam antibiotics target?

A

The septum formation stage of bacterial replication

104
Q

Give an example of a beta 1 selective beta blocker

A

Atenolol

105
Q

Give 2 examples of non-dihydropyranca channel antagonists

A

Verapamil

Diltiazem

106
Q

Explain the mechanism of digoxin

A

Inhibits the Na/K ATPase so the Na/Ca exchanger is used instead
Increased Ca leads to increased cardiac contractility causing a steady beat

107
Q

How do beta blockers affect the RAAS system?

A

They decrease renin levels

108
Q

How do alpha blockers work?

Give a side effect

A

They cause vasodilation which decreases blood pressure

Postural hypotension

109
Q

What is the suffix of a calcium antagonist

2 things it does

A

‘-ipine’

Inhibits muscle and vasodilation

110
Q

What is the suffix of an ACE inhibitor?

A

‘-pril’

111
Q

What is the suffix of an AT receptor blocker?

A

‘-sartan’

112
Q

What drug is used to block Aldosterone?

A

Spironolacetone