202 Core Drugs

Question 1

Core Drug : Diazepam
What class of drug?
Indication?

Answer 1

It is an anxiolytic
Indication - GAD and PD
(not so effective in OCD and PTSD)

Question 2

Core Drug : Chlorpromazine
What class of drug?
Indication?

Answer 2

It is a typical antipsychotic (first one discovered)

Indication - Schizophrenia (primarily + symptoms), also mania

Question 3

Core Drug : Haloperidol
What class of drug?
Indication?

Answer 3

It is a typical antipsychotic (more potent than chlorpromazine)
Indication - Schizophrenia (primarily + symptoms), also acute manic episodes

Question 4

What drugs can cause extrapyramidal symptoms?

Answer 4

Extrapyramidal symptoms are most commonly caused by typical antipsychotic drugs that antagonize dopamine D2 receptors. (E.g. Haloperidol)

Question 5

What are extrapyramidal symptoms?

Answer 5

→ Extrapyramidal symptoms - parkinsonian symptoms, dystonia, akithisia, tardive dyskinesia

Question 6

Core Drug : Risperidone
What class of drug?
Indication?

Answer 6

It is an atypical antipsychotic (Atypicals do not have same extra-pyramidal side effects -lower activity at D2 receptor)
Indication - Schizophrenia, also mania

Question 7

Core Drug : Clozapine
What class of drug?
Indication?

Answer 7

It is an atypical antipsychotic (Atypicals do not have same extra-pyramidal side effects -lower activity at D2 receptor)
It’s activity mainly at D4 receptors (also binds D3, D1, D2, D5), 5HT receptors
Indication - Schizophrenia (+ and - symptoms), also mania

Question 8

Side effects of Clozapine (atypical antipsychotic)

Answer 8

Not extrapyramidal but - weight gain, sedation, hypersalivation, tachycardia, hypotension, neutropenia (needs to be watched - blood tests)

Question 9

Core Drug : Lithium
What class of drug?
Indication?
Positive effects?
Side effects?

Answer 9

antimanic agent - Used for mania and bipolar disorder
Anti-suicidal effects - strong evidence for prevention of relapses of any polarity
Narrow therapeutic index
Blood tests every 3 months for the 1st year
Adverse long-effects on kidney function with excessive levels and risk of lithium toxicity

Question 10

Core Drug : Amitriptyline
What class of drug?
Indication?

Answer 10

Amitriptyline is a type of drug called a tricyclic antidepressant. (1st generation antidepressants)

Question 11

Side effects of tricyclic antidepressants

Answer 11

Constipation, orthostatic hypotension, dry mouth, drowsiness, cardiac toxicity in overdose

Question 12

Core Drug : Fluoxetine
What class of drug?
Indication?

Answer 12

SSRI’s

Used for the treatment of Major depression, OCD, PTSD, Panic, GAD, social anxiety

Question 13

Side effects of SSRIs

Answer 13

Gastro-intestinal symptoms (nausea, diarrhoea), headache, irritability, anxiety, reduction of libido and sexual dysfunction

Question 14

Positive’s of SSRIs

Answer 14

Low toxicity and safe in overdose
Large spectrum of action
Efficacy equal to tricyclics in outpatients

Question 15

SSRI initial treatment phase

Answer 15

most delicate - due to prevalence of side effects over benefit - slow titration

Question 16

Core Drug : Paracetamol
What class of drug?
Good effects?
Mechanism of action?
Dangerous in?
Indication?

Answer 16

Analgesic - Not classically a member of the NSAID group
Minimal anti-inflammatory effects, but good analgesic/ anti-pyretic
Very well-tolerated with almost no contraindications
Mechanism of action is controversial
- Doesn’t bind COX1 or 2; weak inhibitor of prostoglandin
- May inhibit COX3 (CNS only) but relevance controversial
Dangerous in overdose
Indication - mild to moderate pain

Question 17

Core Drug : Ibuprofen
What class of drug?
Good effects?
Mechanism of action?
Indication?

Answer 17

NSAID
Short-term management of pain (and fever)
As anti-inflammatories (?) - gout, inflammatory arthritis, rheumatoid arthritis
NSAID’s All inhibit cyclo-oxygenase

Question 18

NSAID mechanism of action

Answer 18

All inhibit cyclo-oxygenase
Three isoforms
COX-1 - Constitutive expression – all tissues
Stomach, Kidney, Platelets, Vascular endothelium
Inhibition → anti-platelet activity, also side effects
COX-2 – Induced in inflammation (IL-1)
Injury, infection, neoplasia
Inhibition → analgesia and anti-inflammatory actions
COX-3 – CNS only?
May be relevant to paracetamol

Question 19

Indications for NSAID therapy

Answer 19

Short-term management of pain (and fever)
- As mild analgesics (orally and topically)
mechanical pain of all types
minor trauma
headaches, dental pain
dysmenorrhoea
- As potent analgesics (orally, parenterally, rectally)
peri-operative pain
ureteric colic
- As anti-inflammatories (?)
gout
Inflammatory arthritis eg ankylosing spondylitis, rheumatoid arthritis

Question 20

NSAID GI toxicity

Answer 20

In the GI tract prostaglandins E2 and I2 
- Decrease acid production
- Increase mucus production
- Increase blood supply
NSAID inhibition in stomach and duodenum
- Irritation
- Ulcers (gastric 15-30%, duodenal 10%)
- Bleeding
Similar effect in the colon
- Colitis – esp with local preps e.g. rectal diclofenac
Upper GI bleeding
- Relative Risk 4.7 all users
- Azapropazone = 23.4
- Piroxicam = 18.0
- Small differences between others…
Biggest risk factor for GI bleed = previous GI bleed
Also
- Age
- Chronic disease (e.g.rheumatoid disease)
- Steroids

Question 21

NSAID nephrotoxicity

Answer 21

Primarily related to changes in glomerular blood flow
Decreased glomerular filtration rate
Sodium retention
Hyperkalaemia
Papillary necrosis
Acute renal failure 0.5-1%
Avoid or dose adjust in renal failure
Avoid in patients likely to develop renal failure

Question 22

Core Drug : Codeine phosphate
What class of drug?
Indication?

Answer 22

Opioid analgesic

Mild to moderate pain

Question 23

Core Drug : Morphine
What class of drug?
Indication?
Side effects?

Answer 23

Opioid analgesic
Severe pain
Side effects - respiratory depression/airway loss, nausea/vomiting, constipation/pruritis, miosis

Question 24

Core Drug : Pizotifen
Indication?
Side effects?

Answer 24

Prevention of vascular headache, 
Prevention of classical migraine, 
Prevention of common migraine, 
Prevention of cluster headache
Side effects - Appetite increased; dizziness; drowsiness; dry mouth; fatigue; nausea; weight increase

Question 25

Core Drug : Carbamazepine
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 25

Anticonvulsant
Inactivates sodium channels, raises AP threshold and lowers excitability
Used for seizure disorders and neuropathic pain
Side effects - Nausea, vomiting, dizziness, drowsiness, constipation, dry mouth, or unsteadiness may occur.

Question 26

Core Drug : Sodium valproate
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 26

anticonvulsant (or anti-epileptic)
Sodium valproate is an anticonvulsant which elevates GABA levels in the brain.
Used for primary generalized epilepsy
Side effects:
Sedation, Tremor
long term: Hair thinning, Weight gain, Menstrual irregularities, Encephalopathy, Parkinsonism

Question 27

Core Drug : Phenobarbitone
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 27

Barbiturate
All forms of epilepsy except typical absence seizures, also anaesthesia
The primary action of phenobarbital is to enhance the inhibitory actions of gamma-aminobutyric acid (GABA) on neurons

Question 28

Barbiturates are an indirect agonist of what?

Answer 28

GABA(A) - increase the duration of channel openings (anaesthesia, epilepsy treatment)

Question 29

Core Drug : Phenytoin 
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 29

anticonvulsants 
Used for Tonic-clonic seizures (grand mal seizure) , 
Focal seizures
Side effects - 
problems with walking and coordination
slurred speech
confusion
dizziness
trouble sleeping
nervousness
tremors
headache
nausea or vomiting
constipation
skin rash
irregular movement of the eye

Question 30

some anti-epileptic drugs make myoclonic jerks and absences worse - which drugs?

Answer 30

phenytoin*, carbamazepine, gabapentin, pregabalin

*although phenytoin treats tonic clonic seizures so safe to use in status epilepticus

Question 31

Core Drug : Ropinirole 
What class of drug?
Mechanism?
Indication?
Side effects?
Do not give this drug to people who have history of...

Answer 31

Dopamine agonists.
Ropinirole is used alone or with other medications to treat the symptoms of Parkinson’s disease (non-ergot - They have not been associated with a risk of heart damage and can be prescribed)
Side effects: Confusion; dizziness; drowsiness; fatigue; gastrointestinal discomfort; hallucination; movement disorders; nausea; nervousness; peripheral oedema; sleep disorders; syncope; vertigo; vomiting
Do not give this drug to people who have history of gambling due to Dopamine dysregulation syndrome - people complain of impulsive disorders - gambling, online shopping etc

Question 32

What is Dopamine dysregulation syndrome (DDS)?

Answer 32

Dopamine dysregulation syndrome (DDS) is a dysfunction of the reward system observed in some individuals taking dopaminergic medications for an extended length of time. It typically occurs in people with Parkinson’s disease (PD) who have taken dopamine agonist medications for an extended period of time.

Question 33

Core Drug : Levodopa 
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 33

Levodopa is a dopamine precursor used in the management of Parkinson’s disease.
Side effects - nausea, dizziness, headache, insomnia, abnormal dreams, dry mouth, dyskinesia, anxiety, constipation, vomiting, and orthostatic hypotension

Question 34

Core Drug : Selegiline 
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 34

Selegiline is a monoamine oxidase inhibitor used to treat major depressive disorder and Parkinson's.
Side effects - 
dizziness.
lightheadedness.
fainting.
dry mouth.
nausea.
vomiting.
stomach pain.
difficulty swallowing.

Question 35

Levodopa-induced … (LID) is commonly seen in Parkinson’s disease patients treated with levodopa.

Answer 35

Levodopa-induced dyskinesia (LID) is commonly seen in Parkinson’s disease patients treated with levodopa.

Question 36

Core Drug : Entacapone  
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 36

COMT inhibitors
Entacapone prevents the peripheral breakdown of levodopa, by inhibiting catechol-O-methyltransferase, allowing more levodopa to reach the brain.
Entacapone is used in the treatment of Parkinson’s disease as an adjunct to levodopa/carbidopa therapy
Side effects - Nausea, vomiting, diarrhea, unwanted/uncontrolled movements, increased sweating, drowsiness, tiredness, dry mouth, gas, and abdominal pain may occur.

Question 37

Core Drug : Donepezil  
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 37

Cholinesterase inhibitors
Treatment of mild to moderately severe Alzheimer’s dementia (a drug used to improve cognition and behaviour of people with Alzheimer’s, but which does not slow the progression of or cure the disease.)
Side effects - diarrhoea, headache and feeling sick (nausea)

Question 38

Core Drug : Lidocaine  
What class of drug?
Mechanism?
Indication?
Side effects? (injection)

Answer 38

Lidocaine is a local anaesthetic of the amide group (also an antiarrhythmic)
Apply topically
Lidocaine specifically blocks Na+ channels in the inactivated state - raises the threshold, lowers excitability, stopping AP locally
Used for pain relief - topically, dentistry etc - It is also used to treat ventricular tachycardia.
Side effects of injection = 
Low blood pressure (hypotension)
Swelling (edema)
Redness at injection site.
Small red or purple spots on skin.
Skin irritation.
Constipation.
Nausea.
Vomiting.

Question 39

Core Drug : Propofol  
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 39

Anaesthetic
Side effects - Apnoea; arrhythmias; headache; hypotension; localised pain; nausea; vomiting
The GABAA receptor is a target of many general anesthetics, such as propofol

Question 40

Core Drug : Naloxone  
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 40

Opioid antagonist - A medication used to block the effects of opioids. (note - not the same as naltrexone, an opioid antagonist used to help with cravings and prevent drug relapse)
Used for opiate overdose
Side effects - Arrhythmias; dizziness; headache; hypertension; hypotension; nausea; vomiting

Question 41

Naltrexone is used for what?

Answer 41

Opiate antagonist (note - not the same as naloxone) - used as a treatment to reduce alcohol consumption and craving in alcoholics, also smoking cessation

Question 42

Core Drug : Suxamethonium  
What class of drug?
Mechanism?
Indication?
Side effects?

Answer 42

A muscle relaxant used in modern anaesthesia to facilitate rapid sequence endotracheal intubation by providing skeletal muscle relaxation. It is known as a non-depolarising neuromuscular inhibitor.
They are dangerous drugs - muscle paralysis - only administered by experienced people
Side effects - Arrhythmias; bradycardia (may occur with repeated doses); flushing; muscle contractions involuntary; myoglobinaemia; myoglobinuria; post procedural muscle pain; rash