Pharmacology Flashcards
1
Q
What are the 3 major ways that antibiotics can kill bacteria?
A
- Inhibit cell wall synthesis
- Inhibit nucleic acid synthesis
- Inhibit protein synthesis
2
Q
What two types of antibiotics inhibit cell wall synthesis?
A
Glycopeptides, beta lactams
3
Q
What are the 3 types of beta lactams?
A
Penicillins, Cephalosporins, carbapenems
4
Q
Name a glycopeptide antibiotic
A
Vancomycin
5
Q
What is vancomycin used to treat?
A
C diff (Second line), Severe staph infections e.g. MRSA
6
Q
List 3 types of penicillins
A
Benzylpenicillin, flucloxacillin and amoxicillin/ampicillin
7
Q
What is benzylpenicillin used to treat?
A
General resp infections ( pneumonia, strep throat). Also syphilis, gonococcal infection
8
Q
What is flucloxacillin used to treat?
A
Cellulitis and other skin infections (diabetic skin infections, ulcers etc)
Staph Aureus, Strep Pyogenes
9
Q
What is ampicillin/amoxicillin used to treat?
A
Community Acquired pneumonia, COPD exacerbations, UTIs (2nd line)
10
Q
What are the three generations of cephalosporins?
A
1st gen: Cephalexin
2nd gen: Cefuroxime
3rd gen: Ceftazidime= Ceftriaxone
11
Q
What are cephalosporins used to treat?
A
Chlamydia and Gonnohea
Staph Aureus, streptococci, nisseriae, haemophillus, coliforms
12
Q
Name a carbapenem antibiotic
A
Imipenems, ertapenems
13
Q
What are the cautions of glycopeptides?
A
Caution in renal impairment, history of deafness, pregnancy
14
Q
What are the contraindications of penicillins?
A
Penicillin hypersensitivity
15
Q
What are the side effects of benzylpenicillin and flucloxacillin?
A
Hypersensitivity reactions
16
Q
What are the side effects of ampicillin/amoxicillin?
A
Nausea, vomitting
17
Q
What are the four ways that antibiotics can inhibit nucleic acid synthesis?
A
Inhibit folate synthesis
Inhibit DNA gyrase
Bind to RNA polymerase
DNA strand breaks
18
Q
Which antibiotics inhibit folate synthesis?
A
Trimethoprim, sulfamethoxazole, and co-trimoxazole (both combined)
19
Q
Which antibiotics inhibit DNA gyrase?
A
Fluoroquinolones: Ciprofloxacin
20
Q
Name an antibiotic that binds to RNA polymerase
A
Rifampicin
21
Q
Which antibiotics causes DNA strand breaks?
A
Nitrodimazoles: metronidazole
22
Q
What is trimethoprim used to treat?
A
UTI, prostatitis, acute/chronic bronchitis
Co-trimoxazole= PCP treatment and prophylaxis
23
Q
What is Ciprofloxacin used to treat?
A
Acute pyelonephritis, gastroenteritis
24
Q
What is rifampicin used to treat?
A
Mycobacteria- used as part of the quadruple TB treatment
25
What are nitrodimazoles used to treat?
Anaerobes, parasites
26
What are the cautions of Trimethoprim?
Pregnancy as inhibit folate synthesis
27
What are the side effects of trimethoprim?
Hyperkalaemia, depression of haematopoesis
| Co-trimoxazole= Hyperkalaemia, Rash
28
What are the cautions of Fluoroquinolones?
Epilepsy, D6PD deficiency, myasthenia gravis
29
What are the contraindications of rifampicin?
Jaundice
30
What are the side effects of rifampicin?
Orange discolouration of saliva and urine, anorexia, nausea and vomitting, haemolytic anaemia
31
What are the contraindications of metronidazole?
Interaction with alcohol= profuse vomitting
32
What are the four types of antibiotics that inhibit protein synthesis?
Chloramphenicol
Macrolides
Tetracyclines
Aminoglycosides
33
List two macrolide antibiotics
Clarithromycin and erythromycin
34
List two tetracycline antibiotics
Tetracycline, doxycycline
35
List two aminoglycoside antibiotics
Gentamycin and streptomycin
36
What are macrolides used to treat?
General alternative to penicillin
37
What are tetracyclines used to treat?
Broad spectrum antibiotic.
| Acne, Chlamydia, SIADH
38
What is gentamycin used to treat?
Staph, aureus, gram -ve bacilli, used for severe sepsis
39
What are the contraindications of tetracyclines?
Children <12 due to deposition in bone and teeth leading to hypoplasia, renal disease
40
What are the contraindications of aminoglycosides?
Myasthenia gravis
41
What antibiotic is usually used to treat non severe community acquired pneumonia?
Amoxicillin +/- clarithromycin
42
What antibiotic regime is usually used to treat TB?
RIPE= Rifampin (6), Isoniazid (6) , Pyrazinamide (2), and Ethambutol (2)
43
What antibiotic is usually used to treat atypical community acquired pneumonia?
Clarithromycin
44
What antibiotic is usually used to treat cellulitis?
Flucloxacillin
45
What antibiotic is usually used to treat infrequent exacerbations of COPD?
Amoxicillin/ Clarithromycin/ Doxycline
46
What antibiotic is usually used to treat UTIs?
Trimethoprim/ Nitrofurantoin
47
What antibiotic is usually used to treat hospital acquired pneumonia?
Co-amoxiclav
48
What antibiotic is usually used to treat acute pyelonephritis?
Co-amoxiclav/ Ciprofloxacin
49
What antibiotic is usually used to treat gonorrhoea?
Ceftriaxone (IM)
| Azithromycin (PO)
50
What antibiotic is used to treat chlamydia?
Doxycycline/ Azithromycin (PO)
51
What antibiotic is used to treat syphilis?
Benzylpenicillin
52
What antibiotic is used to treat gastroenteritis?
(Campylobacter) Clarithromycin
| (Salmonella/ Shigella) Ciprofloxacin
53
What antibiotic is used to treat C.Difficile?
1st: Metronidazole
2nd: Vancomycin
54
What antibiotic is used to treat appendicitis?
Ceftriaxone and metronidazole
55
What is pharmodynamics?
How the drugs affects the body
56
What can drugs target?
Receptors, enzymes, transporters and ion channels
57
Name some types of receptors
Ligand-gated ion channels
G protein coupled receptors
Kinase-linked receptors
Nuclear receptors
58
What are the two types of G protein coupled receptors?
M3R and beta-2adrenoreceptors
59
What is potency?
A measure of how well a drug works
60
What is EC50?
The concentration of a drug that gives half the maximal response
61
What is an agonist?
A compound that binds to a receptor and activates it
62
What is an antagonist?
A compound that reduces the effect of an agonist
63
What is competitive antagonism?
When an antagonist competes with the agonist to bind receptors, thereby preventing agonists from having an effect.
64
What is non-competitive antagonism?
When an antagonist binds near the receptor causing a conformational change, so the agonist cannot activate the receptor
65
What effect does competitive antagonism have?
It causes the dose response curve to shift right, meaning that more agonist is required to illicit the same response
66
What effect does non-competitive antagonism have?
A right shift and down of the dose response curve= meaning that even more agonist is required to illicit the same response
67
What are the two types of cholinergic receptors?
Muscarinic ACh receptor and Nicotinic ACh receptor
68
What is affinity?
Describes how well a ligand binds to the receptor (shown by both antagonist and agonist)
69
What is efficacy?
Describes how well a ligand activates the receptor (only agonists show efficacy)
70
What is signaling transduction and amplification?
When a ligand binds at a receptor it sets off a signalling cascade which is then amplified. This can determine how powerful a response is
71
What is allosteric modulation?
When binding of an allosteric ligand to a receptor can affect an agonists effect on a receptor either positively (allosterically) or negatively (orthosterically)
72
What is inverse agonism?
When a drug binds to the same receptor as an agonist and induces a pharmacological response opposite to that agonist
73
What is tolerance?
The reduction in drug effect over time. It is seen with continuous, repeated high concentration over drug over time
74
Give an example of a selective drug
Salbutomol is a selective B2 adrenoceptor agonist (whereas isoprenaline is non selective so it activates both B1 and B2 receptors)
75
How do NSAIDs work?
They inhibit the enzyme cyclooxygenase by competitive inhibition, which is the enzyme that converts arachidonic acid to prostaglandin H2
76
Are NSAIDs selective?
Most are selective- celecoxib is COX2 selective
| Aspirin is non-selective so acts on both COX1 and COX2
77
Where is COX found?
```
COX1= Normally and widely around the body
COX2= Induced and found in inflammation only
```
78
What is the role of uniporters?
Use energy from ATP to pull molecules in
79
What are symporters?
Use the movement of one molecule to move another molecule in against its concentration gradient
80
What are antiporters?
One substance moves against its conc gradient using energy from the second substance moving down its gradient (opposite directions)
81
What is the route of formation of dopamine?
L-Tyrosine forms L dopa
| L dopa then forms dopamine via dopa decarboxylase
82
What is synergy?
Where the actions of two drugs combine, such as paracetamol and codeine to increase analgesic effect
83
What are some patient risk factors for drug interactions?
```
Polypharmacy
Old age
Genetics
Hepatic disease
Renal disease
```
84
What are some drug risk factors for interactions?
Narrow therapeutic index
Steep dose/response curve
Saturable metabolism
85
What is saturable metabolism?
When after a certain point, the drug cannot be metabolised anymore
86
What things can affect drug absorption?
Motility, Acidity, Solubility, Complex formation, enterocyte action
87
What interactions affect motility?
Antibiotics often cause diarrhoea, so interacts with the absorption of the oral contraceptive
88
What can affect the solubility of a drug?
Eating high fat food whilst taking a fat soluble drug will cause the drug to dissolve and thus not be absorbed
89
What four major things affect pharmokinetics?
Aborption
Distributions
Metabolism
Excretion
90
How might distribution of a drug be affected?
Protein binding in the plasma
91
How might metabolism of a drug be affected?
Things affecting Cytochrome P450
92
How might excretion of a drug be affected?
Renal excretion is pH dependent= Weak bases are cleared faster if urine is acidic, and vice versa
93
Name some acidic drugs
Aspirin, Ibuprofen, paracetamol, warfarin
94
Name some basic drugs
Amphetamine, atropine, propranolol, salbutamol
95
Name some ways to avoid drug interactions
Prescribe rationally= BNF
Medicines information service
Technological mechanisms
96
Name some foods that have drug interactions
Avocado, grapefruit juice, garlic, Soya, Ginger
97
Name 3 drug targets
Receptors, enzymes, transporters, ion channels
98
The action of a drug can be either receptor-related or tissue-related, which of these do the principles of affinity and efficacy influence? (1) What do agonists / antagonists show?
Affinity and efficacy relate to receptors
| Agonists show affinity & efficacy / antagonists show affinity only
99
Describe the difference between tolerance and desensitisation?
Tolerance - reduction in drug effect over time (continuously repeated high conc)
Desensitisation - receptors become degraded / uncoupled / internalised
100
What class of drug is Candesartan?
Angiotensin II Receptor Blocker
101
Which common condition often diagnosed in childhood is a contraindication of beta-blockers and why?
Asthma
| Beta-Blockers cause bronchoconstriction
102
Approximately 60% of the body is comprised of water. In an average 70Kg male this constitutes 42 L of water. Approximately how many liters of water would you expect to find in the following compartments of this patient: Intracellular, Extracellular, Plasma?
- Intracellular ~ 28L (2/3),
- Extracellular~ 14L (1/3).
- Plasma ~3 L (a component of the extracellular compartment)
103
What are the 4 stages of Pharmacokinetics?
- Absorption
- Distribution
- Metabolism
- Excretion
104
What is pharmacokinetics?
The fate of the drug in the body after administration
105
What is a first order reaction?
Where rate of diffusion is directly proportional to the concentration of the drug
106
What is a second order reaction?
Where Rate of diffusion is directly proportional to the square of the conc of the drug
107
What is a third order reaction?
Where Rate of diffusion is directly proportional to the cube of the conc of the drug
108
What is a zero order reaction?
Where rate of diffusion is unrelated to the conc of the drug
109
What are the three compartments of the body?
Plasma
Interstitial
Intracellular
110
What are the 5 ways that a drug can move between compartments?
```
Simple diffusion
Facilitated diffusion
Active transport
Extracellular spaces
Non-ionic diffusion
```
111
What is the relationship between pH, and the ionisation of drugs?
When pH is increased- weak acids become more ionised, and weak bases become less ionised
and Vice Versa
112
What is pinocytosis?
A form of carrier mediated entry into the cytoplasm. Usually involved in the uptake of endogenous macro molecules.
113
What is bioavaiability?
Amount of drug taken up as a proportion of the amount administered
114
What route of administration gives the highest bioavailability?
Intravenous
115
List some routes of administration
Oral, IV, IM, Transcut, Intrathecal, sublingual, inhalation, topical, rectal
116
What can vary the bioavailability of oral medication?
Surface area of gut, pH of gut, stomach motility, diarrhoea etc.
117
Which route of administration works the fastest?
Intravenous
118
Why is it necessary for an oral drug to be lipid soluble?
To allow for it to be absorbed in the gut
119
What is volume of distribution?
The total amount of drug in the body/ the concentration of drug in the plasma
120
In which component are proteins/large molecules active?
Plasma
121
In which component are water soluble molecules active?
Plasma and interstitial compartment
122
In which component are lipid soluble molecules active?
Intracellular fluid
123
What is clearance?
The volume of plasma that can be completely cleared of drug per unit time
124
What is kidney clearance?
rate of appearance in urine/ plasma concentration
125
What substance is used as a marker in the kidneys?
Creatinine
126
What is renal blood flow?
1l/min
127
What properties would make a drug more likely to be eliminated by the kidney?
Water soluble and small molecules
128
What is hepatic extraction ratio?
The proportion of a drug that can be removed by one passage through the liver
129
What is high first pass metabolism?
A high hepatic extraction ratio, meaning that a high proportion is removed by one passage through the liver
130
What is the function of phase I reactions?
To make drugs more reactive = expose OH or other reactive sites
131
What enzyme is used in phase I reactions?
Cytochrome P450 enzymes
132
Give some examples of phase I reactions
Hydroxylation, delalkylation, deamination, hydrogen removal, reduction, hydrolysis
133
What is the aim of phase II reactions?
Glucuronidation= Make the molecule hydrophillic
134
What enzyme is used in phase II reactions?
Glucuronosyltransferase (UGT)
135
What is enterohepatic circulation?
When some drug from the bile rediffuses from the gut back into the blood, and is then reconjugated
136
Why are IV infusions used?
```
Enable steady state plasma
Enables accurate drug delivery
Fast
100% Bioavailability
Useful if oral medication isn't possible
```
137
When does steady state normally occur?
4-5 half lives
138
How do you calculate loading dose?
Loading dose = steady state x volume of distribution
139
How do you calculate rate of elimination during a steady state?
Clearance x drug conc between peaks and troughs
140
How do you calculate steady state?
Rate of infusion/ Clearance
141
How is insulin administered?
Sub cutaneously
142
What is the oral bioavailability of morphine?
50%= due to first pass metabolism of the liver
143
What percentage of the population cannot metabolism morphine?
10%
144
Name some naturally occurring opioids
Morphine, Codeine
145
Name some synthetic opioids
Pethidine, fentanyl, alfentanil
146
Name an opioid antagonist
Nalaxone
147
How do opioids work?
Opioids block the descending pain transmission
They use the natural opioid receptors (G proteins) and inhibit the release of pain transmitters at the spinal cord and midbrain, and modulate pain perception in higher centres
148
What are the opioid receptors?
MOP, KOP, DOP, NOP
149
Where are opioid receptors found?
Midbrain, spine, GI tract, and breathing centre
150
What is dependence?
Psychological (craving of euphoria) and physical dependence
151
What are some side effects of opioids?
Respiratory depression, Sedation, Nausea and vomiting, Constipation, Itching. Immune suppression, Endocrine effects
152
How do you treat opioid induced respiratory depression?
Airways, breathing, circulation
| IV Naloxone and titrate to effect
153
List some local anaesthetics
lidocaine and procaine
154
How do local anaethetics work?
Local anesthetics block the conduction of the nerve by blocking Na+ channels thereby preventing the depolarisation of the nerve and the propagation of the action potential
155
Why do patients often get constipated with opioid use?
Opioid receptors are located in the GI tract
156
How long does opioid withdrawal take?
It begins at 24 hrs and lasts about 72 hrs
157
Which branch of the nervous system is voluntary and what neurotransmitter(s) does it use?
Somatic
| Uses acetyl choline
158
Which branch of the nervous system is involuntary and what neurotransmitter(s) does it use?
Autonomic
| Uses Ach and noradrenaline
159
What are the two branches of the autonomic nervous system?
Parasympathetic and sympathetic
160
Is the post-synaptic ganglion closer to the spinal cord in the sympathetic or the parasympathetic system?
```
Sympathetic= Ganglion lies closer to the spinal cord
Parasympathetic= Ganglion lies closer to the effector organ
```
161
What type of receptors are used in parasympathetic and sympathetic systems?
Both use nicotinic for the first synaptic ganglion
Parasympathetic uses muscarinic receptors in effector organs
Sympathetic uses alpha or beta receptors in effector organs
162
What neurotransmitters does the parasympathetic and sympathetic systems use?
Both use ACh in the first synaptic ganglion
Parasympathetic also uses ACh in effector organ
Sympathetic uses noradrenaline at effector organ
163
What are NANCs and where are they found?
Non-adrenergic, non-cholinergic autonomic transmitters
| Found in the enteric nervous system
164
Briefly explain what happens at a neuromuscular junction
1. Choline acetyl transferase enzyme makes ACh
2. ACh is packaged into a vesicle
3. The vesicle is exocytosed and ACh is released
4. ACh acts on receptor
5. ACh is broken down by acetylcholinersterase
165
What is botulinum toxin and how does it work?
It prevents vesicle fusion thus inhibiting the release in ACh release.
It results in paralysis, and is used for spasticity, and cosmetically (botox)
166
How does nerve gas cause paralysis?
It irreversibly inhibits acetylcholinesterase meaning ACh remains indefinately
167
Where are M1 receptors found?
Mainly in the brain
168
Where are M2 receptors found?
The heart- their activation slows the heart
169
Where are M3 receptors found?
Glandular and smooth muscle. Cause bronchoconstrictition, sweating, salivary gland secretion
170
Where are M4/5 receptors found?
Mainly in the CNS
171
How does atropine help in cardiac arrest and bradycardia?
It blocks M2 receptors so will oppose the parasympathetic nervous system and stop slowing of the heart
172
List some functions of the parasympathetic nervous system
```
Rest and digest
Constricts pupils
Stimulates tears and salivation
Lowers heart rate
Reduces respiration
Contract bladder
Erection
```
173
List some functions of the sympathetic nervous system
```
Fight or flight
Dilates pupils
Inhibits tears and salivation
Increases heart rate and respiration
Relaxes bladder
Ejaculation
```
174
What is the consequence of Alpha 1 receptor innervation?
Contraction of smooth muscles (pupils, blood vessles), Vasoconstriction, increased blood pressure
175
What is the consequence of alpha 2 receptor innervation?
Lowers blood pressure, Increased glucagon release, reduced insulin
176
What is the consequence of beta 1 receptor innervation?
Chronotropic and inotropic effects on heart
| = Increases heart rate and myocardial contractility
177
What is the consequence of beta 2 receptor innervation?
Relaxes smooth muscle (vasodilation, bronchodilation)= lowers blood pressure
178
What is the consequence of beta 3 receptor innervation?
Enhances lipolysis, relaxes detrusor muscle
179
Which beta blockers are beta 1 selective?
Atenolol, bisoprolol, metoprolol
180
What is the effect of adrenaline?
Targets blood vessels (alpha-1), heart (Beta-1) and bronchial smooth muscle (Beta-2), causing vasoconstriction, positive inotropic effects and bronchodilation
181
What type of drug is atenolol?
B1 selective Beta blocker
182
List a medication a that is derived from plants.
```
Morphine= Poppy
Atropine= Deadly nightshade
```
183
Name a drug that was derived by chance
Penicillin and sildenafil
184
Why are sulphonamide nuclei added to drugs?
It is rigid and unreactive, so adds stability to the drug
185
Name a drug that was derived by rational receptor approach
Proponalol
| Cimetidine
186
What are sterioisomers?
Molecules that have chiral carbons, and are mirror images of one another= rotate plane polarised light in an opposite direction
187
What are the two types of stereoisomers and which is used more?
D (S form) or L (R form). Biological systems use L-amino acids (R form).
188
Who invented the first vaccine and what was the vaccine for?
```
Edward Jenner (in 1796)
Smallpox
```
189
List some recombinant proteins in clinical drug use
```
Insulin
Erythropoietin
Growth hormone
Interleukin 2
Gamma interferon
Interleukin 1 receptor antagonist
```
190
What is
| Combinatorial chemistry?
Biochemical modification of natural products
191
What is Combinatorial biosynthesis?
Large enzyme complexes generate natural products, and then manipulate biosynthetic machinery to generate structural analogues
192
Briefly explain antibody based immunotherapy
Serum from patients who have had a certain disease can be taken and their antibodies can be isolated and given to other patients as a treatment
193
Briefly explain monoclonal antibody formation
Mouse is immunised against specific antigen. B cells are isolated to check they are producing antibodies. If it is, B cells in the spleen are removed and then cultured along with myeloma tumour cells. Solution is added to fuse the B cells with the tumour cells to produce hybridomas that can divide indefinitely and produce antibodies. The hybridomas are then cloned. Antibodies are produced and then used for clinical purposes
194
What are humanised antibodies?
Chimeric (humanised) antibodies have a mix of human and mouse antibody chains
195
How does azathioprine prevent DNA formation?
Blocks incorporation of thiopurine analogues into the DNA structure, causing chain termination and cytotoxicity
196
What is high-throughput screening?
Robotics and data processing software to screen millions of chemical, genetic or pharmacological tests to find targets. It looks at the biological activity of compounds
197
What is an adverse drug reaction?
An unwanted or harmful reaction following administration of a drug or combination of drugs under normal conditions of use and is suspected to be related to the drugs
198
What is the different between adverse drug reactions and side effects?
Adverse drug reactions have to be negative
Side effects can be beneficial
Generally minor and predictable ADR's are called side effects
199
What can make a patient more susceptible to an ADR?
```
Age- elderly or neonates
Gender- More common in females
Pregnancy- Negative effect on baby etc
Disease- Liver or renal in particular
Drug interactions
Diet or alcohol intake changes
Genetics
```
200
What is a hyper-susceptibility effect?
A very small amount of a drug below the theraputic range, that still causes an ADR
201
What are collateral effects?
ADRs that occur within the theraputic range
202
What are toxic effects?
ADRs that occur above the theraputic range
| Can occur if dose is too high or drug excretion is reduced
203
What are some drug risk factors for ADRs?
Steep dose-response curve
Low therapeutic index
Commonly causes ADRs
204
What are the Rawlins Thompson categories for adverse drug reactions?
```
Augmented
Bizarre
Chronic
Delayed
End of use
Failure of therapy
```
205
What are augmented adverse drug reactions?
Commonest and predictable
An extension of the clinical effect
Dose related and self-limiting
206
Give an example of an augmented adverse drug reaction
Examples include diuretic causing dehydration, anticoagulants causing bleeding, hypertensive drug causing hypotension.
207
What are bizarre adverse drug reactions?
Not predictable and not dose dependent ABRs
208
List some categories of time dependent reactions
```
Rapid reactions
First dose reactions
Early reactions
Intermediate reactions
Late reactions
Delayed reactions
```
209
Give an example of a drug that has a delayed reaction
Thalidomide
210
What are end of treatment adverse drug reactions?
Drug reactions that occur after drug withdrawal e.g. withdrawal
211
Give an example of a bizarre drug reaction
Anaphylaxis
212
What does DoTS stand for (regarding ADRs)?
Dose relatedness
Timing
Susceptibility
213
What are chronic adverse drug reactions?
Drug reactions that occur after long term treatments of a drug
214
Give an example of a chronic drug reaction
Steroids can cause osteoporosis
215
What is a failure adverse drug reaction?
When a medication fails to work properly- oral contraceptive etc.
216
What is the yellow card scheme?
A form to report adverse drug reactions
217
What are the clinical features of anaphylaxis?
CVS- Vasodilation, increased vascular permeability, lowered BP, angio-oedema
Respiratory- Dyspnoea due to bronchoconstriction, mucus production
Skin- Urticaria Rash, swelling
GI- Pain, vomiting
218
How is anaphylaxis treated?
Commencement of basic life support- Airways, Breathing, Circulation
Stop drug if infusion
Adrenaline IM 500 micrograms Or 300 micrograms in epi-pen
High flow oxygen
IV anti histamine (Chlorphenamine 10mg)
IV hydrocortisone (100-200mg)
219
When do ADRs need to be reported via the yellow card system?
All suspected ADRs for new medicines
All ADRs in children
All serious reactions to include fatal, life threatening, disabling, or incapacitation ADRs
220
What is non-immune anaphylaxis?
Due to direct mass cell degranulation
Doesn't require prior exposure
Clinically identical to immune anaphylaxis
221
What is the effect of adrenaline?
Vasoconstriction- increases peripheral vascular resistance to increase BP
Stimulation of beta1- adrenoceptors- positive inotropic and chronotropic affects on heart
Attenuates anaphylactic response from mast cells
Reduces oedema
222
What type of hypersensitivity reaction is anaphylaxis?
Type 1- IgE mediated
223
```
A drug given through IV route is assumed to have a bioavailability of..
A) 50%
B) 75%
C) 100%
D) 10%
```
Correct answer= C
224
What is meant by the term parenteral administration?
The drug is delivered to the systemic circulation, bypassing the GI tract (e.g. IV, IM, Sub Cut)
225
What is meant by the term enteral administration?
The drug is delivered via the GI tract (e.g. oral, rectal)
226
What is meant by the term pharmacodynamics?
What a drug does to the body
227
Why should you not give propanolol to patients with asthma?
It is a non-selective Beta blocker, so also affects B2= causing bronchoconstriction
228
NAPQI is a toxic metabolite that builds up in the liver and causes acute liver necrosis. Levels of which antioxidant are depleted in paracetamol OD?
glutathione
229
What drug is used to treat paracetamol OD?
Acetylcysteine
230
Activation of which type of adrenoreceptor leads to tachycardia, increased myocardial contractility and renin release?
B1
231
```
Which of the following processes do beta lactam antibiotics intefere with...
A) Bacterial protein synthesis
B) Bacterial cell wall synthesis
C) Bacterial nucleic acid synthesis
D) Viral protein synthesis
```
Correct answer= B
232
```
Which of the following is an irreversible enzyme inhibitor...
A) Enalapril
B) Aspirin
C) Ibuprofen
D) Salbutamol
```
Correct answer= B
233
What is the first line for s. pyogenes?
Penicillin
234
Name a beta lactamase inhibitor antibiotic?
Clavulanic acid, sulbactam, and tazobactam
235
What is co-amoxiclav?
amoxicillin and clavulanic acid
236
Briefly explain how ramipril works
Ramipril targets Angiotensin Converting Enzyme (ACE), and competitively inhibits it. This inhibits synthesis of potent vasoconstrictor peptide angiotensin II leading to vascular smooth muscle relaxation and vasodilatation.
Overall effect: Reduced blood pressure
237
When should renal function be monitored when using a ACE inhibitor?
Renal impairment — monitor renal function 1–2 weeks after starting an ACE-inhibitor, after each dose increase, and regularly throughout treatment
238
Why do Afro-Caribbean patients respond less well to ACE inhibitors?
Angiotensin converting enzyme (ACE) inhibitors, β blockers, and angiotensin receptor antagonists are generally less effective as monotherapy in black hypertensives, because of the tendency towards a low renin state and a lower cardiac output, with increased peripheral resistance.
239
What is St. Johns Wort?
St John's wort is a herbal remedy that has been used for hundreds of years to treat mental health problems. Today it is mainly used as an over-the-counter remedy to treat mild and moderate depression, and sometimes seasonal affective disorder (SAD), mild anxiety and sleep problems.
240
List some medications that St. Johns Wort is known to interact with?
Alprazolam (Xanax), Some contraceptives, Aminolevulinic acid, Amitryptiline, Cyclosporine, Digoxin, Fenfluramine, Medications changed by the liver, Antidepressants , Medications for HIV/AIDS, Medications for pain (Narcotic drugs), Warfarin
241
In a patient with a new diagnosis of depression what class of drug would initially be used?
SSRIs are usually the first choice medication for depression because they generally have fewer side effects than most other types of antidepressant
242
How does methotrexate work for inflammation?
Methotrexate has antiinflammatory and immunosuppressive effects which are due to inhibition of inflammatory mediators such as IL-6, IL-8 and tumour necrosis factor
243
Why is Folic Acid given to RA patients on Methotrexate?
Methotrexate (As a cancer treatment) acts by inhibiting the conversion of folic acid to tetrahydrofolate therefore preventing protein synthesis. As this is not required in rheumatoid arthritis, the patient should take folic acid to prevent deficiency
244
Doxazosin and Tamsulosin are both alpha 1-blockers and both used for benign prostatic obstruction, which receptors do they act on?
They are highly selective for alpha-1 adrenoceptors which are found mainly on smooth muscle, including blood vessels and urinary tract
Blocking these receptors therefore causes relaxation, so vasodilation and reduced resistance to bladder outflow
245
An elderly gentleman needs cataract surgery and is taking Tamsulosin for his lower urinary tract symptoms (LUTS), why is it important that he lets his surgeon know that he is taking it?
It may slightly lower his blood pressure, so is important to consider during the anaesthetics
246
The patient complains of dizziness when standing up quickly after taking Tamsulosin with his breakfast, how would you advise him?
Start taking the medicine at bedtime to minimise the impact of the dizziness (although if they get up from the bed at night time, they will need to be careful)
247
How should alendronate be taken?
In the morning, at least 30 minutes before eating with plenty of water. The patient should remain upright for 30 minutes after taking.
248
Why would a patient be taking letrozole?
For early and locally advanced oestrogen-receptor positive breast cancer
249
How would you treat a P. aeruginosa infection?
Ciproflolaxin
250
What is Clenil Modulite?
Beclomethosone (ICS)- given for prophylaxis of asthma attacks
251
What is salbutamol?
A SABA. Given for acute flares of asthma/ after exercising.
252
What class of drug is contraindicated with non DHP CCBs?
Beta blockers (precipitate heart failure)
253
What medication is given in PCI?
CABG
| Aspirin + Prasugrel (or clopidogrel if on anticoagulant)
254
What medication is given in fibrinolysis for STEMI?
Alteplase + aspirin + ticagrelor
255
When is fibrinolysis indicated in STEMI?
If over 120 mins but below 12 hrs
256
What is the immediate treatment of NSTEMI?
Aspirin+ fondaparinux
257
What is the typical basic dual antiplatelet therapy for STEMI/NSTEMI?
Aspirin + ticagrelor
258
What is the higher risk dual antiplatelet therapy for NSTEMI/STEMI?
Aspirin + prasugrel
259
What is the long term management post MI?
```
ABAAC
AceI/ARB,
Beta Blocker
Aspirin
Atorvstatin
Clopidogrel / prasugrel/ ticagrelor
```
260
What is prescribed for heart failure?
DABAD
1. Diuretics (loop)= furosemide 40mg
2. ACEi
3. Beta blocker= Carvedilol 3.125 mg
4. Aldosterone antagonist= Spironlactone 25 mg
5. Digoxin
261
What condition are beta blockers contraindicated for?
Asthma
262
What would you do for a non haemodynamically stable AF?
DC Cardioversion
263
What would you do for a haemodynamically stable AF with a rate over 200bpm?
DC Cardioversion
264
What would you do for a haemodynamically stable AF with a rate under 200bpm, and onset less than 48hrs?
Rhythm control+ LMWH
- Electrical DC cardioversion
- Amiodarone
265
What would you do for a haemodynamically stable AF with a rate under 200bpm, and onset morethan 48hrs?
Rate Control
| - Beta blocker or CCB
266
What does a CHA2DS2-VASc score of over 1(males) or over 2(females) indicate?
Anticoagulate with DOAC
267
What is not indicated in heart failure
- Ramipril
- Furosemide
- Verapamil
- Carvedilol
- Spironlactone
Verapamil
268
What type of drug is Carvedilol?
Beta blocker
269
What are the ADPr antagonists?
Clopidogrel
Prasugrel
Ticagrelor
270
What is the main side effect of aspirin?
GI irritation (Give with PPI)
271
What is the main caution with digoxin?
Narrow therapeutic window
272
What clotting factors are inhibited by warfarin?
10, 9, 7, 2
273
What is the target INR?
2-3
274
What do DOACs inhibit?
Factor Xa (prothrombin cannot be converted to thrombin)
275
When is fondaparinux prescribed?
Immediate treatment of NSTEMI
276
How is heparin typically administered?
SubCut (5000 units SC daily)
277
When is fresh frozen plasma given?
TTP
278
What are the K+ sparing diuretics?
Spronlactone, amiloride
279
What drug class is flecianide and when is it given?
Na+ channel blocker
| Block channels responsible for depolarisation
280
When would EPO often be given?
Chronic disease
| In Jehovah's witnesses if blood products are refused
281
What is the immediate management of a STEMI?
```
MONA
Morphine
Oxygen
Nitrate
Aspirin 300mg
```
282
A patient comes in with massive bleed. He is currently on warfarin. How is this reversed in an acute setting?
Prothrombin complex concentrate and vitamin K
283
Which P2Y12 inhibitor is reversible?
Ticagrelor
284
What are whole blood products indicated for?
Massive blood loss
285
What blood products would be given for DIC?
First line- Platelets
| Second line- Cryoprecipitate
286
What blood product would be given first line for warfarin overdose?
Prothrombin complex concentrate
287
What blood product would be given for TTP?
Fresh frozen plasma
288
What blood product would be given for VWD?
Cryoprecipitate
289
How is DKA monitored/treated?
FIG-PICK
- Fluids
- Insulin; actrapid
- Glucose monitoring
- Potassium monitoring
- Infection- find and treat
- Chart fluid balance
- Ketone monitoring
290
What would you prescribe for stable angina?
1. Beta blocker/ calcium channel blocker
| 2. Nitrate
291
What is the first pharmacological intervention for type 2 diabetes?
Metformin
292
What are the main side effects of metformin?
Nausea and diarrhoea
293
How does metformin work?
Decrease hepatic glucose production
| Increase muscle glucose uptake and utilisation
294
How is thyrotoxic storm treated?
```
Fluids
Propranolol
Digoxin
Hydrocortisone
Carbimazole
```
295
What are the methods of treating hyperthyroidism?
- Radioactive iodine
- Thionamides
- Surgery
- Beta blockers
296
How is hypothyroidism treated?
Levothyroxine for secondary and primary causes
297
How would acute hypothyroidism be treated?
Liothyronine IV (T3)
298
What class is metformin?
Biguanide
299
What class is gliclazide?
Sulphonyurea
300
What class is dapagliflozin?
SGLUT2 Inhibitor
301
What class is pioglitazone?
Thiazolidinedione
302
What class is sitagliptin?
DPP4 Inhibitor
303
```
Which of these is the priority in the treatment of a DKA
A) Potassium monitoring
B) Insulin administration
C) Ketone monitoring
D) Fluid resuscitation
E) Glucose monitoring
```
D
304
A 41-year-old lady has recently been started on carbimazole for Grave's disease. She attends her GP as she believes she is having side effects from the medication.
Which of these would not be a potential side effect of taking carbimazole?
A) Palpitations
B) Constipation
C) Hair loss
D) Fatigue
A
305
What surgical treatments could be given for OA?
- Arthoscopy for loose bodies in joints
- Osteotomy- removal of bone
- Arthroplasty (joint replacement)
- Fusion of joint
306
What is the first line treatment for OA?
Education, Exercise, weight loss, physio
| - Initially paracetamol
307
What should be co-prescribed with NSAIDs?
Lansoprazole (15mg daily)
308
Should NSAIDs or paracetamol be given first in degenerative arthritis?
Paracetamol
309
What are the contranidications of NSAIDs?
Renal impairment
Heart failure
Liver failure
Peptic ulcers
310
How quickly should treatment for rheumatoid arthritis start?
Within 3 weeks of symptoms
311
Give an example of an Anti-TNF
Adalimumab
Infliximab
Entercept
312
Give an example of an ANTI-CD20
Rituximab
313
Give an example of an Anti-IL6
Sarliumab
| Tocilzumab
314
Give an example of a JAK inhibitor
Tofactinib
| Barictinib
315
What drug gives temporary male infertility?
Sulfasalazine
316
What is the first line treatment for RA?
Methotrexate, leflunomide or sulfasalazine
317
What are the side effects of methotrexate?
Pneumonitis, pulmonary fibrosis, liver toxicity, pancytopenia, tetratogenic
318
What must be coprescribed with methotrexate?
Folic acid
319
What are the side effects of lefunomide?
Increased BP, Peripheral neuropathy, liver toxicity
320
How does methotrexate work?
Dihydrofolate reductase inhibitor, prevents cell replication and production of inflammatory mediators
321
What is the second line treatment for RA?
Combination of= Methotrexate, leflunomide or sulfasalazine
322
What is the third line treatment for RA?
Methotrexate plus biological DMARD (Usually TNF Inhibitor such as adalimumab)
323
What type of drug is a rituximab?
Anti-CD20
324
What is the fourth line treatment for RA?
Methotrexate plus rituximab
325
What is the treatment for spondyloarthropathies
1. Exercise +NSAID
2. DMARD, Anti-TNF
3. Secukinumab (ank spon), ustekinumab (Psoriatic)
326
Are paracetamol or NSAIDs prescribed first in spondyloarthropathies??
NSAIDs
327
What does HRT increase the risk of?
Breast cancer and CVD
328
What is denosumab prescribed for?
Osteoporosis (3rd line after adcal, bisphophonates and HRT)
| = It is a MAb to RANKL
329
What is secukinumab prescribed for?
Ank spon
330
What is ustekinumab prescribed for?
Psoriatic arthritis
331
How is osteomalacia treated?
Vit D (50000 IU before tapering down to 800IU daily) +/- Calcium
332
How often is zoledronic acid given for osteoprosis?
IV once yearly
333
What are the common side effects of allopruinol?
Gout if given during acute flare, skin rash, Stevens-Johnson syndrome
334
What drug would be suitable first line for a patient with RA
- Topical diclofenac
- Leflunomide
- Etanercept
- IM methylprednisolone
Leflunomide
335
What are the side effects of Isoniazid?
Hepatitis, neuropathy
336
What are the side effects of pyrazinamide?
Gout, rash, nausea, myalgia
337
What are the side effects of ethambutol?
Visual changes (optic neuritis)
338
How does citalopram affect an ecg?
It prolongs the QT interval
339
What should be avoided when on metronidazole?
Alcohol
340
What antibiotic causes "red man" syndrome?
Vancomycin
341
What antibiotic can cause tendon rupture?
Ciproflolaxin
342
How do you treat undiagnosed dyspepsia?
1 month of PPI (Omeprazole)
343
How do you treat GORD?
2 months of PPI
344
What is the triple therapy for h. pylori?
PPI (omeprazole) + Clarithromycin + metronidazole or amoxicillin
345
How do you treat a non-variceal upper GI bleed?
Adrenaline injection at bleeding site on endoscopy+ thermal/mechanical ligation + IV PPI for 72 hrs
346
How do you treat a variceal upper GI bleed?
Terlipressin + prophylactic Abx + band ligation (oesophageal varices)
347
How do you treat choleystitis?
IV Abx, IV fluids, analgesia, cholecystectomy
348
How do you treat acute cholangitis?
Fluid resus, IV abx, analgesia, ERCP
349
How do you treat chronic pancreatitis?
Analgesia, enzyme replacement therapy
350
What hepatitis is best treated with pegylated interferon alpha?
B (can use in D but poor evidence)
351
What hepatitis is common in East-Asia?
Hep E
352
How do you treat hepatic encephalopathy?
Lactulose
353
How do you treat a mild flare of UC?
1. Topical 5-aminosalicylate
2. Oral 5-aminosalicylate
3. Oral steroids
354
How to you treat a severe flare of UC?
1. IV steroids
2. Ciclosporin
3. Surgery
355
How do you maintain remission after a mild flare of UC?
5-Aminosalicylate
356
How do you maintain remission after a severe flare of UC?
Azathioprine or mercaptopurine
357
How do you treat a flare of Crohns?
1. Steroids
2. 5-Aminosalicylate
3. + Methotrexate
4. + Infliximab
358
How do you maintain remission of Crohns?
1. Azathioprine or mercaptopurine
| 2. Methotrexate
359
What is tenesmus?
Cramping rectal pain where the patient feels that they need to pass stool
360
What is the first line treatment for asthma?
SABA
361
What is the second line treatment for asthma?
SABA+ ICS
362
What is the third line treatment for asthma?
SABA+ICS+LABA
363
What is the fourth line treatment for asthma?
SABA+ICS+LABA+Ipratropium
364
What classifies as severe asthma?
- Inability to complete sentances in one breath
- Resp rate over 25
- PEF 33-50%
- Heart rate over 110
365
What classifies as life threatening asthma attack?
Severe plus
- o2<92%
- Normal paCO2
- Altered consciousness
366
What classifies as near fatal asthma?
Life threatening plus hypercapnia (type 2 resp failure)
367
What is the treatment of acute asthma attack?
O SHIT ME
1. Oxygen if needed= Severe
1. Salbutamol = Moderate/ Severe
1. (Hydrocortisone or) prednisolone= Moderate/Severe
2. Ipratropium= Add on for life threatening
3. Theophylline
3. Magnesium sulphate
4. Escalate
368
What is the best treatment for COPD?
Smoking cessation
369
Give an example of a LAMA
Tiotropium
| Ipratropium
370
What is the first line treatment for COPD?
SABA
371
What is the "triple therapy" for COPD?
```
LABA= Salmeterol
LAMA= Tiotropium
ICS= Beclomethasone
```
372
What are the rules of oxygen therapy?
- Over 15 hrs a day
- Patients with pO2 <7.3 kpa
- No smoking !
373
What is the main treatment for a COPD exacerbation that isn't due to bacteria?
Prednisolone
374
What are the classic symptoms of glucocorticoids?
CUSHINGOID MAP
Cataracts, ulcers, Striae, Hypertension, Incfection risk, Necrosis of bone, growth restriction, Osteoporosis, increased ICP, Diabetes, Myopathy, Adipose tissue hypertrophy, pancreatitis
375
How do you treat mild CAP(curb 65 0-1)?
Oral Amoxicillin 5 days
376
How do you treat moderate CAP (CURB65 2)?
Admit, IV fluids, analgesia, oxygen
| IV Co-amoxiclav or Tazocin + Clarithromycin
377
How do you treat severe CAP (CURB65 3+)?
Admit, IV fluids, analgesia, oxygen
| IV Co-amoxiclav or Tazocin + Clarithromycin
378
What should be co-prescribed with isoniazid?
Pyridoxine (Vitamin B6)
379
How do you treat a haemodynamically stable patient with PE?
DOAC (Apixaban or rivaroxaban)= 3 months if known cause, 6 months if unknown cause
380
How do you treat a haemodynamically unstable patient with PE?
Thrombolysis with alteplase
381
If a Wells score is over 4, how should you investigate?
CTPA
382
If a Wells score is under 4, how should you investigate?
Plasma D dimer
383
How would you generally initially treat a severe asthma attack?
Nebulised salbutamol and PO prednisolone
384
How would you generally initially treat a life threatening asthma attack?
Nebulised salbutamol and tiotropium and PO prednisolone
385
How do you treat stress incontinence?
Pelvic floor training
Duloxetine (SNRI)
Surgery
386
How do you treat urge incontinence?
Bladder retraining
Antimuscarinics= oxybutynin
Mirabegron
387
What is the treatment scheme of BPH?
1. Alpha 1 antagonist e.g. doxazosin, Tamsulosin
2. 5 Alpha reductase inhibitor e.g. finasteride
3. TURP
388
What is the main side effect of doxazosin/ tamsulosin?
Hypotension
389
How do you treat migraine?
Triptan (CI in CHD and hypertension) + simple analgesia = NSAID or paracetamol
= Prophylaxis beta blocker
390
How do you treat tension-type headache?
Simple analgesia, stress relief
391
How do you treat cluster headache?
Subcut sumatriptan + high flow O2
| = Beta blocker or tricyclic antidepressant for prophylaxis
392
How do you treat trigeminal neuralgia?
Carbamazepine
| = Calcium channel blocker for prophylaxis
393
How do you treat temporal arteritis?
High dose Prednisolone and aspirin
394
How do you treat generalised epilepsy?
1. Sodium valproate
| 2. Lamotrigine/ Carbamazepine
395
How do you treat focal epilepsy?
1. Lamotrigine/ Carbamazepine
| 2. Levetiracatam/ Sodium valproate
396
How do you treat absence epilepsy?
1. Sodium valproate
| 2. Ethosuximide
397
How do you treat myoclonic epilepsy?
1. Sodium valproate
| 2. Lamotrigine
398
In which types of epilepsy should carbamazepine be avoided?
Absence and myoclonic
399
What is status epilepticus?
Continuous seizure lasting over 5 minutes or repeated seizures with no recovery of consicousness in between
400
How do you treat status epilepticus?
1. Benzodiazepine (diazepam or lorazepam)
2. Phenytoin, sodium valproate, levetircetam, phenobarbital
3. Induction of general anaesthetic with propofol
401
How do you treat meningitis?
- IM Benzylpenicillin in community
- IV ceftriaxone or cefotaxime + amoxicillin if over 50 or very young
- IV dexamethosone to reduce chance of long term consequences
402
How do you treat encephalitis?
IV aciclovir stat
