S3 Pharm Flashcards
What is the MOA of sodium valproate?
Weak inhibitor of enzymes that deactivate GABA (GABA transaminase) OR blocking the reuptake of GABA into glia cells or pre-synaptic neurons
What is sodium valproate used for?
Anticonvulsant
Mood stabilizer - Bipolar disorder
What are the side effects of sodium valproate?
Abdo pain
Headaches
Confusion
Folate anatagonist
What is the MOA of lithium?
Block NMDA receptors, therefore reducing Ca2+ inflow into the post-synaptic neuron, thus reducing the excitatory effects of glutamate.
What is lithium used for?
Anticonvulsant
Mood stabilizer - Bipolar disorder
What are the side effects of lithium?
Kidney damage Abdo pain Weight gain Tremor Sexual problems
What is the MOA of lamotrigine?
Blocking sodium and calcium channels but does not have effects on GABA metabolism.
What is lamotrigine used for?
Anticonvulsant
Mood stabilizer - Bipolar disorder
What are the side effects of lamotrigine?
headache, dizziness; blurred vision, double vision; tremor, loss of coordination; dry mouth, nausea, vomiting, stomach pain, diarrhea; fever, sore throat, runny nose; drowsiness, tired feeling; back pain; or. sleep problems (insomnia).
What is folate used for?
The production and maintenance of new cells, for DNA synthesis and RNA synthesis, and for preventing changes to DNA. It plays a crucial role in the closure of the anterior and posterior neuropores.
What is contained in folate supplements?
Folinic acid and THF.
What is the MOA for NSAIDs?
Inhibition of COX, thus inhibit the production of prostaglandins (anti-inflammatory and antipyretic effects) and thromboxanes (anti-platelet effect).
Anti-inflammatory effects reduce pain.
What is the MOA for ibuprofen?
Weak COX-1 inhibitor
What is the MOA for paracetamol?
Selective COX-2 inhibitor
What is the MOA of opioids?
Morphine and the codeine in co-codamol bind to opioid receptors (mainly μ):
Inhibition of adenylyl cyclase, thus reducing intracellular cAMP.
Open potassium channels, causing hyperpolarisation.
Inhibit calcium channel opening, therefore reduce neurotransmitter release.
What is the MOA of gabapentin?
Increases GABA synaptic concentration, by acting as a calcium channel modifier.
What are the common side effects of opioids?
sedation, dizziness, nausea, vomiting, constipation, physical dependence, tolerance, and respiratory depression
What are the common side effects for gabapentin?
abnormal eye movements clumsiness or unsteadiness. constipation. diarrhea. difficulty speaking. drowsiness or tiredness. dry mouth. nausea.
What is gabapentin used for?
Anticonvulsant, used to treat neuropathic pain
What is the MOA of lidocaine?
Blocks sodium channels, thus preventing the generation of action potentials in the pain fibres.
What are the main side effects of lidocaine?
Hypotension Oedema Redness at injection site. Small red or purple spots on skin. Skin irritation. Constipation. Nausea. Vomiting
What is the MOA of timolol?
Beta-blocker
Reduce intraocular pressure by decreasing aqueous humor.
Increases the peripheral resistance and so there is less blood supply to the ciliary body, thus reduction in the production of aqueous humor.
What is the MOA of beinzolamide?
Carbonicanhydrase inhibitor
Reduce intraocular pressure by decreasing aqueous humor production/secretion.
Inhibition of this enzyme in the ciliary processes slows the formation of bicarbonate, and reduces sodium and fluid transport
What is Amoxicillin?
Antibiotic (B-lactam ring). Given after 72 hours if the infection has not settled down
What is the MOA of tissue plasmogen activator?
Inactivates thrombin and ADP.
tPA is a protease that cleaves plasminogen to form plasmin.
Plasmin, in turn, cleaves fibrin and other coagulants to degrade thrombi (fibrinolysis).
What are the side effects of tPA?
nausea, vomiting, hypotension dizziness, mild fever, allergic reactions
What is the MOA of warfarin or heparin?
Inhibits the function of coagulating factors in clot formation
What is the MOA of aspirin or clopidegrol?
Inhibit the function of platelets in clot formation
What are the side effects of warfarin?
unusual bruising nosebleeds. bleeding gums. bleeding from cuts that takes a long time to stop. heavier than normal menstrual or vaginal bleeding. pink or brown urine. red or black stools. coughing up blood.
What are the side effects of heparin?
easy bleeding and bruising;
pain, redness, warmth, irritation, or skin changes where injected;
itching of your feet
bluish-colored skin.
What are the side effects of aspirin?
Ringing in your ears, confusion, hallucinations, rapid breathing, seizure;
severe nausea, vomiting, or stomach pain;
bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
fever lasting longer than 3 days;
swelling, or pain lasting longer than 10 days.
What are the side effects of clopidegrol?
Headaches or dizziness. nausea. diarrhoea or constipation. indigestion (dyspepsia) stomach ache or abdominal pain. nosebleeds. increased bleeding or bruising
What is the MOA of benzodiazepines?
Binds to α subunit on GABA-A receptor, thus causing the ion channel to open. This causes an influx of Cl- ions, resulting in hyperpolarisation, thus reducing anxiety. Benzodiazepines also increase the affinity of the receptor for GABA
What is the MOA of SSRIs?
Selectively block serotonin reuptake transporter proteins, thus increasing the concentration of serotonin in the synaptic cleft.
What is the MOA of SNRIs?
Blocks serotonin and noradrenaline reuptake transporter proteins, thus increasing their concentration in the synaptic cleft
What is the MOA of pregabalin?
Increases GABA synaptic concentration.
What are the side effects of diazepam?
drowsiness. tiredness or fatigue. muscle weakness. inability to control muscle movements (ataxia) headache. tremor. dizziness. dry mouth or excessive saliva.
What are the side effects of sertraline?
drowsiness or tiredness; insomnia or agitation; indigestion, nausea, diarrhea, loss of appetite; sweating; tremors or shaking; sleep problems (insomnia); decreased sex drive
What are the side effects of venlafaxine?
nausea, vomiting, diarrhea; changes in appetite or weight; dry mouth, yawning; dizziness, headache, anxiety, feeling nervous; fast heartbeats, tremors or shaking; sleep problems (insomnia), strange dreams, tired feeling; vision changes; increased sweating
What are the side effects of pregabalin?
ataxia, blurred vision, constipation, diplopia, dizziness, drowsiness, fatigue, headache, peripheral edema, tremor, weight gain, visual field loss
What is the MOA of methylpresnisolone?
Corticosteroid
Anti-inflammatory effects
Inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives
What are the side effects of methypresnisolone?
headache. nausea and vomiting. weight gain. confusion, excitement, and restlessness. swelling of your ankles, feet, or hands. skin problems
What is the MOA of IFN-B?
Decrease T-cell proliferation. Decrease T-cell activation. Decrease T-cell migration
What are the side effects of IFN-B?
headache. vaginal bleeding or spotting between menstrual periods. tight muscles. weakness. changes in sex drive or ability (in men) change in coordination
What is the MOA of glatiramer acetate (copaxone)?
Binds to MHC-2 to prevent binding of antigens. Competes with MBP for binding to T cell receptor. Inhibits activation of MBP reactive T cells
What are the side effects of glatiramer acetate (copaxone)?
Injection site reactions nausea, vomiting, chills, joint aches, body aches, neck pain, back pain,
What is the MOA of fingolimod (gilenya)?
Blocks sphingosine 1-phosphate receptor-1 (S1P receptor), thus trapping lymphocytes in lymph nodes
What are the side effects of fingolimod (gilenya)?
Headache. Abnormal liver tests. Diarrhea. Cough. Flu. Inflammation of the sinuses (sinusitis) Back pain. Stomach-area (abdominal) pain.
What is the MOA of natalizumab (tysarbi)?
Monoclonal antibody that binds to α4β1 integrin on WBC. This prevents the binding of the α4β1 integrin to the VCAM-1 selectin, thus preventing the migration of WBC across the BBB
What are the side effects of natalizumab (tysarbi)?
Sudden fever or severe headache; confusion, memory problems, or other changes in your mental state; weakness on one side of your body; vision changes, eye pain or redness; problems with speech or walking; trouble using your arms and legs.
What is the MOA of terifluromide (aubagio)?
Inhibit mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). This decreases T-cell function.
What are the side effects of terifluromide (aubagio)?
Liver problems, influenza, hair loss or thinning hair, nausea, diarrhea, burning or prickly feeling in your skin numbness or tingling in your hands or feet s.
What is the MOA of dimethyl fumarate (BG-12)?
Activates Nrf-2 transcriptional pathway, thus reducing inflammation
What are the side effects of dimethyl fumarate (BG-12)?
flushing and feeling hot. gastrointestinal upset decrease in white blood cells. rash. increased levels of liver enzymes. ketones and protein in urine.
What is the MOA of reserpine?
Irreversible VMAT blocker. This causes the cytoplasmic monoamines in the presynaptic nerve terminal to be broken down by MAO and COMT, leading to LONG-LASTING DEPRESSION!
What are examples of irreversible MAO inhibitors?
Iproniazid
Phenelzine
Tranylcypromine
What is an example of a reversible MAO inhibitors?
Moclobomide
What are examples of TCAs?
Amitriptyline
Clomipramine
What are examples of SNRIs?
Venlafaxine Imipramine
What are examples of SSRIs?
Sertraline Fluoxetine Paroxetine Citalopram Escitalopram Fluvoxamine
What is the MOA of mirtazapine?
α2 adrenergic receptor antagonist. As a result the negative feedback loop to inhibit the release of noradrenaline is blocked, thus increasing the release of noradrenaline and serotonin.
What are the side effects of mirtazapine?
Drowsiness. Weight gain. Dry mouth. Increased appetite. Constipation. Lack of energy. Weakness. Dizziness
What is the MOA of atypical antipsychotics?
- Blockade of dopaminergic D2 receptors in the ventral striatum, alleviating positive symptoms of schizophrenia such as hallucinations and delusions.
Blockade of serotonergic 5-HT2 receptors in the mesocortical tract, causes an excess of dopamine, resulting in an increase in dopamine transmission, and an elimination of core negative symptoms.
What is the MOA of levodopa?
Precursor of dopamine.
Decarboxylated into dopamine after crossing BBB.
Stimulate dopaminergic receptors.
What is the MOA of benserazide/carbidopa?
Peripherally-acting DOPA decarboxylase inhibitor.
Reduces peripheral side effects of levodopa.
cannot cross the BBB and so doesn’t prevent the effects of levodopa in the brain
What are the side effects of co-beneldopa?
Anxiety; appetite decreased; arrhythmia; depression; diarrhoea; hallucination; movement disorders; nausea; parkinsonism; postural hypotension; sleep disorders; taste altered; vomiting
What is the MOA of Selegiline?
Irreversible MAO-B inhibitor. Increases the amount of dopamine in the pre-synaptic neuron after reuptake. This allows more dopamine to be repackaged into vesicles via VMAT, for subsequent release.
What are the side effects of Selegiline?
Dizziness, abdominal pain, dry mouth, nausea, stomach upset, trouble sleeping, and headache
What is the MOA of chlorpromazine and Haloperidol?
Dopamine receptor antagonist. Serotonin (5-HT) receptor antagonist. Histamine (H1) receptor antagonist.
α-adrenergic receptor antagonist. Muscarinic (M1) receptor antagonist.
What does dopamine receptor antagonism lead to? (schizophrenia)
Reduced positive symptoms
What does serotonin receptor antagonism lead to? (schizophrenia)
elimination of negative symptoms
What does histamine receptor antagonism lead to? (schizophrenia)
Sedation
What does adrenergic receptor antagonism lead to?
Lower BP
What does muscarinic receptor antagonism lead to?
anticholinergic side effects: blurred vision and dry mouth
What are examples of atypical antipsychotics?
Risperidone
Clozapine
Quetiapine
Olanzopine
What causes elevated serum prolactin levels?
Antagonism of dopamine receptors in the tuberoinfundibular pathway
What causes parkinsonian symptoms?
Antagonism of dopamine receptors in the nigrostriatal pathway
What causes weight gain?
Antagonism of histamine H1 and serotonin 5-HT2c receptors plus effects on leptin
What causes a deterioration in working memory?
Antagonism of dopamine receptors in the mesocortical pathway
What causes blurred near vision?
Antagonism of muscarinic M1 acetylcholine receptors
What causes sedation?
Antagonism of histamine H1 and alpha-adrenergic receptors
What drugs can be used for induction of general anaesthesia?
Propofol
Ketamine
Etomidate
Sodium Thiopental
What is the MOA of propofol?
Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation.
positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.
GABA-A receptor agonist
What are the side effects of propofol?
ast or slow heart rate, high or low blood pressure, injection site reactions (burning, stinging, or pain), apnea, rash, itching.
What is the MOA of Ketamine?
NMDA receptor antagonist
What drugs can be used for the maintenance of anaesthsia?
Isoflurane Sevoflurane Desflurane Fentanyl Morphine Propofol Atracurium Pancuronium Suxamethomium (succinylcholine)
What is the MOA of isoflurane?
It is an inhaled volatile anaesthetic agent, used for the maintenance of anaesthesia
GABA-A and glycine agonist
NMDA antagonsit
What are the side effects of isoflurane?
respiratory depression, hypotension, arrhythmias. Shivering, nausea, vomiting
What is the MOA of fentanyl or Morphine?
Strong agonist at the μ-opioid receptor. Upon binding, it inhibits adenylate cyclase which causes an inhibition in the release of nociceptive substances such as substance P, GABA, dopamine
What is the MOA of atracurium?
Muscle Relaxant. Non-depolarising neuromuscular blocking agent. Block ACh receptors at the neuromuscular junction. Spontaneously hydrolysed in plasma (alkali conditions brought about by respiratory alkalosis).
What is the MOA of pancuronium?
Muscle Relaxant. Long-acting non-depolarising neuromuscular blocking agent. Block ACh receptors at the neuromuscular junction.Eliminated from the body via renal excretion and metabolism in the liver.
What is the MOA of suxamethomium?
Muscle Relaxant. Depolarising neuromuscular blocking agent. Mimicks ACh without being broken down by acetylcholinesterase (AChE), leading to desensitization of the neuromuscular junction. broke down by butyrylcholinesterase (BuChE) instead
What are the side effects of atracurium?
skin flushing or redness. injection site reactions. hives. itching. wheezing. shortness of breath. allergic reactions. inadequate musculoskeletal block.
What are the side effects of pancuronium?
increased saliva, skeletal muscle weakness, drooling, rash, bronchospasm, flushing, redness, low blood pressure
What are the side effects of suxamethomium?
Malignant hyperthermia, muscle pains, acute rhabdomyolysis with high blood levels of potassium, transient ocular hypertension, constipation and changes in cardiac rhythm
What drugs can be used for the reversal of general anaesthetic?
Neostigmine
Glycopyrrolate
Atropine
What is the MOA of neostigmine?
Cholinesterase Inhibiting Drug. Blocks AChE, thus increasing the concentration of ACh in the neuromuscular junction, therefore increasing muscular contraction. Increases effects at both nicotinic and muscarinic receptors
What are the side effects of neostigmine?
salivation, increased mucus, muscle twitching, bowel or abdominal cramps, nausea, vomiting, diarrhea, decreased pupil size
What is the MOA of glycopyrrolate?
Muscarinic Receptor Antagonist. This limits parasympathetic effects caused by neostigmine such as bradycardia
What are the side effects of glycopyrrolate?
Decreased sweating. Dry mouth. Constipation. Mild dizziness. Drowsiness. Headache. Loss of taste. Nervousness.
What is the MOA of atropine?
Inhibit muscarinic acetylcholine receptors
limits parasympathetic effects caused by neostigmine
Can cross BBB
What are the side effects of atropine?
dry mouth, blurred vision, sensitivity to light, lack of sweating, dizziness, nausea, loss of balance, hypersensitivity reactions