People and Illness Flashcards
methylphenidate
- ritalin
- stimulant
- acts primarily on the dopamine transporter, and has little effect on synaptic release
- blocks DA & NA re-uptake via transporter
- Net result = INCREASE IN DOPAMINE
- first line pharmacological treatment for children with ADHD
- Fast onset - effect is evident within 30 minutes of the dose.
- Appetite suppression and sleep disturbance
Dexamphetamine
- releases DA stored in presynaptic vesicles
- also blocks dopamine transporter protein (inhibits reuptake) NET RESULT IS INCREASE IN DOPAMINE
- d-form of AMPHETAMINE
- given when ADHD symptoms are unresponsive to a maximum tolerated dose of methylphenidate or atomoxetine or when epilepsy deteriorates
Atomoxetine
- Noradrenaline Reuptake inhibitor
- Enhances noradrenaline transmission in the prefrontal cortex area
- Second-line drug for ADHD treatment
- good alternative for children struggling with side effects of methylphenidate/dexamphetamine
- Once daily or BD dosing.
- 6 week onset, no drug holidays
SE include hepatic impairment -> important to monitor LFTs
Clonidine
- α-2 adrenergic receptor agonist
- reduces NE release from terminals
- used as third line drug for ADHD
Psychostimulants
- methylphenidate
- dexamphetamine
Psychostimulants (ADHD) side effects
- Affect growth – suppress appetite
- Parents recommended to give a solid breakfast
before giving medication
- Monitor weight closely - Affect sleep
- BP and HR irregularities
- Drug holidays possible – medication can be stopped over weekends/holidays to allow child to catch up with growth
Guanfacine
- α-2 adrenergic receptor agonist
- enhances prefrontal cortical regulation of attention and impulse control
- used in late teens for ADHD
- increase incrementally to prevent sedation and tiredness
Citalopram
SSRI
- 1st line treatment for depression
- Block 5HT reuptake, 4-5 weeks to have an effect
- 33% response rule
Fluoxetine
SSRI
Sertraline
SSRI
Amitriptyline
TCA
- second line treatment for depression
- Block 5HT, NA reuptake
- can cause arrhythmias
- act act mAChR and have anticholinergic effects (you can see, pee, shit or spit)
Phenelzine
- MAOi
- 3rd line antidepressants
- Block MAO-A, MAO-B – breaks down 5HT, NA, DA in CNS
- can cause Hypertensive crisis; ‘cheese reaction’
Isocarboxid
- MAOi
- 3rd line antidepressants
- Block MAO-A, MAO-B – breaks down 5HT, NA, DA in CNS
- can cause Hypertensive crisis; ‘cheese reaction’
Rituximab
Monoclonal antibody against CD20 (exclusively expressed on B cells. Used to treat B cell lymphoma
Bevacizumab
- Monoclonal antibody VEGF inhibitor
- binds to VEGF and inhibits it from binding to VEGF receptors
- Angiogenesis inhibitors (tyrosine kinase inhibitors) are also ATP-mimetics
Ipilimumab
- Monoclonal antibody that blocks CTLA-4
- In cancer, CTLA-4 is upregulated on T cells, and acts as an ‘off switch’
- blocking CTLA-4 allows reactivation of T cells
- this is an IMMUNE CHECKPOINT INHIBITOR
NB: can cause ulcerative colitis due to T cell activation in the gut
Nivolumab
- Monoclonal antibody that blocks PD-L1
- PD-L1 upregulated in cancer to prevent destruction by T cells
- Blocking PD-L1 on tumours prevents this masking to the immune system
Pembrolizumab
- Monoclonal antibody that blocks PD-1
- PD-1 is a receptor expressed on T cells
- PD-L1 is the ligand for PD-1 – functions as an immune checkpoint
- PD-L1 upregulated in cancer to prevent destruction by T cells
- Blocking PD-L1 on tumours prevents this masking to the immune system
Imatinib
- inhibits Abl
- functions as a specific inhibitor of a number of tyrosine kinase enzymes
- ATP mimetic
- binds to the ATP binding site and stabilizes the inactive, non-ATP-binding form of BCR/ABL
- prevents tyrosine autophosphorylation
- Used to treat Chronic Myeloid Leukaemia (philadelphia translocation produces constitutively active tyrosine kinase BCR-ABL gene)
Enzalutamide
- hormone therapy for men with advanced prostate cancer
- AR signalling inhibitor
- normally effective but splicing mutations can occur that result in constitutive activity, which cannot be inhibited by Enzalutamide as the AR does not even require
androgen binding for action
naloxone
– opioid antagonist
- can reverse heroin overdose if administered quickly
Drugs used to manage alcoholism
naltrexone
disulfiram
acamprosate
Disulfiram
disruption of normal alcohol metabolism.
produces an irreversible inhibition of ADH enzyme
produces an adverse
disulfiram–alcohol reaction that may persist for 30 min to several hours
Symptoms include flushing, headache, nausea and vomiting, sweating, hypotension and tachycardia.
Acamprosate
- used to manage alcohol withdrawal
- GABAA receptor desensitization due to chronic alcohol excess (tolerance) results in unopposed excitatory neurotransmission with withdrawal
- acamprosate enhances GABA signalling at GABAA receptors
Diazepam
- benzodiazepine
- anxiety-reducing, hypnotic, sedative, and anticonvulsantdrug
- also used used for the treatment of benzodiazepine dependence due to its low potency
Vemurafenib
- oral tyrosine kinase inhibitor of the oncogenic BRAF V600 protein kinase
- selectively binds to the ATP-binding site of BRAF (V600E) kinase and inhibits its activity
- used to treat BRAF V600 mutation‑positive unresectable or metastatic melanoma
- this inhibits tumour growth
IFN-α
- used in the treatment of hematologic malignancies and solid tumors
IFN-α can:
1) directly inhibit proliferation of normal and tumor cells
2) down-regulate oncogene expression
3) induce tumor suppressor genes –> contribute to antiproliferative activity
4) increase MHC class I expression, which can enhance immune recognition
IL-2
promotes expansion of tumour-specific T cells.
Crizotinib
anti-cancer drug acting as an ALK inhibitor, approved for treatment of some non-small cell lung carcinoma
