Documentos de Académico
Documentos de Profesional
Documentos de Cultura
Two factors
Blood flow
By
Both above are lipid soluble, cross BBB, not suitable in children as
produce drowsiness
Carteolol
Levobunolol
Metipranolol
Side eects
Blepharoconjunctivitis
Acetazolamide
Dorzolamide
Brinzolamide
Acetazolamide
Periodic paralysis
Absent seizure
Trabecular outflow
Cholinomimetics
Pilocarpine: direct acting, short acting
Shlemms canal
Uveoscleral outflow
Prostaglandin F2 alpha
Travoprost
Unoprostone
Epinephrine
Dipivefrine
Prostaglandins
PGE1
PGE2
Dinoprostone
Enprostil
Rioprostil:
PGF2 alpha
Latenoprost
Bimatoprost
Travoprost
Unoprostone
Vasodilation
Anti aggregatory
Epoprostenol
Treprostinil
Beroprost
Ilioprost
WHO class 2
Sildenafil
Or
Ambresentan
WHO class 3
PGI2
WHO class 4
Combination
Leukotriene antagonist
Leukotriene receptor blockers
Zafirleukast
Monteleukast
Long term therapy causes Churg Strauss syndrome
Headache, eosinophilia, vasculitis
?
PAF
Platelet activating factor
PAF antagonists
Useful for acute pancreatitis
Lexipafant
Apafant
Ulinastatin
Trypsin inhibitor
Severe sepsis
Rupatidine is a 7th generation anti histamine which has anti PAF activity
Thromboxane A2
Platelet aggregation
Sultroban
Daltroban
Losartan
Vapiprost
Picotamide
Blocks Cox 1
Anti platelet
Serotonin
Pr synaptic
5HT 2A/2C
Clozapine
Risperidone
Olanzapine
5HT3
Blockers are
Ondensetran
Granisetran
5HT4
Pro kinetic
Diarrhea
Cisapride
Mosapride
Tegaserod
SSRI
5HT4
Diarrhea
In addition
Platelet function aected
Bleeding disorder
Fluoxetine
Longest acting
Thus some missed dose will not cause SSRI discontinuation syndrome
Fluvoxamine
Shortest acting
Paroxetine
Usually SSRI don't cause wt gain but this causes wt gain
Highly teratogenic
Citalopram
And it's derivative escitalopram are highly selective
Setraline
All SSRI prone for drug interaction but least chance with this drug
CPM
Cyclizine
Meclizine
Second generation
Terfenadine, fastest
Astemazole, slowest
Ebastine
Alzheimer's disease
Cholinergic enhancement
Tacrine
Donepezil
Rivastigmine
Galantamine
Eptastigmine
Paromomycin( aminoglycoside)
Miltefosine( oral)
Sitamaquine( oral )2
Bapineuzumab: monoclonal Ab
A ( amyloid)
Antioxidants
Vitamin E , D
Selegiline
Acetyl L carnitine
Anticholinergic
Most important is atropine
Blocks only muscarinic receptors
Anti secretory
M1 blocker
Pirenzipine
Telenzepine
Anti spasmodic
Dicyclomine
Anti spasmodic
Intestinal colic
Side effect of constipation
Darifenacin
Solefinacine
By relaxing the GIT smooth ms causes constipation
Thus used in diarrhea and diarrhea type IBS
Used in control of over active bladder
Quaternary
Glycopyrrolate
Pre anesthetic medication
To control tracheo bronchial secretion
It is lipid insoluble, no CNS adverse affect
Vesico selective
M3 receptors
Oxybutynin
Flavoxate
Tolterodine
All cause retention
Thus treatment of
Urge Incontinence
Neurogenic bladder due to spina bifida
Nocturnal enuresis
Darifenacin and solifenacin will act here as well non selectively
Merabegron
3 agonist
Relax detrusor, over active bladder
Sibutramine is used for obesity, 3 agonist
Antidepressant for stress incontinence: Duloxetine, SNRI
Also used for fibromyalgia, chronic neuropathic pain
Similarily Venlafaxine SNRI is used
It's side effect is sustained HT
Antiparkinsonism( drug induced)
Trihexphenidyl( benzhexol)
Procyclidine
Biperiden
Benztropine
Acting on pulmonary system
Atropine
Non selective
It also blocks muco ciliary clearance
Ipratropium bromide
Selective
No effect on muco ciliary clearance
Thus good drug for COPD
Aclidinium bromide is a new drug
Cardiovascular
Achievement of symptomatic bradycardia and heart block
Eye
M3 receptor
Paralysis of circular ms
Leads to cycloplegia and Mydriasis
Differentiate with alpha 1 agonist, will cause Mydriasis, no
cycloplegia
If Mydriasis along with loss of light reflex: anticholinergic
Anticholinergic drugs are CI in glaucoma as problem with drainage as
the iris circular ms paralyses
Mydriatics
Atropine, 1% , less than 5 years, 1 week
Homatropine 2% drops, 5-8 years, 1-2 days
Cyclopentolate 1% drops, 8-20 years,
Tropicamide 1% drops, adult, 3-6 hours, fastest and shortest
CNS
Hyoscine/ scopolamine
CNS depressant
Although atropine is stimulant
Hyoscine used in lie detection and motion sickness
M and H1 receptors involved
Thus promethazine can also be used
Sea sickness: longer acting 1st generation, cyclizine,
Mountain sickness: Acetazolamide
Motion sickness: Hyoscine
Morning sickness: doxylamine, promethazine
Doxylamine is an anti histamine
Pyridoxine given in combination coz it is antiemetic
Pyridoxine should not be given to Parkinson pt who is on levodopa
therapy as it is a coenzyme
Glandular
Decreased bronchial secretion, salivation, sweating
Children with hyperthermia, absolute CI
Relative CI in elderly with BPH
Piribidil
D2 and D3 agonist
Used for Parkinson
Also used for cognition and memory
Not used any more
Drugs having anticholinergic activity
1. TCA
Amitryptaline and imipramine have highest activity
2. Anti psychotics
Thioridazone( conventional)
D2 blocker
Thus
Galactorrhea and EPS
If eps is drug induced, give trihexphenidyl
So since thioridazone itself has anti cholinergic activity, very less EPS
side effects
clozapine, atypical antipsychotic
Sialorrhea: pillow wet syndrome
3. Skeletal ms relaxant
Pancuronium
Gallamine
If these are used as ms relaxant, no need of giving glycopyrrolate
4. Class 1a anti arrhythmic drugs
Disopyramide
Unsafe in elderly as BPH
5. 1st generation H1 blocker
Promethazine
6. Others
Amantadine
Meperidine aka pethidine
CI in MI pt as causes tachycardia due to anti cholinergic activity
Pentazocine is also an opioid which is CI in MI but that is due to
sympathetic stimulation
Amantadine
Only for influenza A
Oseltamivir/ zenamivir is used for both A and B?
Amantadine has
Anticholinergic
Dopaminergic agonist
NMDA antagonism: used in Parkinson, major side effect is ankle
edema and levido reticularis( net like rashes)
Q. Parkinson pt develops
Erythromelalgia: pain on walking, tenderness on palpation,Vasospasm
Side effect of bromocriptine( ergot D2 agonist)
Other are
Pergolide: causes cardiac valvular fibrosis
Cabergoline
Non ergot D2 agonist for Parkinson
Pramipixole
Ropinirole, also used for restless leg syndrome
Both above causes psychotic side effects
Excess sexual desire, kleptomania
Rotigotine: transdermal patch for parkinson
4 amino pyridine
Aka dalfampridine
Used in Multiple sclerosis for improving walking
Also used in lambert eaton type of MG
Multiple sclerosis
Disease modifying drugs
Interferon 1A and 1B
Interferon alpha is for antiviral activity, hepatitis b and c
Y is for chronic Granulomatous disease
Glatiramer acetate
Natalizumab : monoclonal Ab, acting against alpha 4 integrin
Given parenteral once a month
Max given for 18 months
Will cause PML
Mitoxantrone: antibiotic anti cancer drug
Causing cardiac failure
Fingolimod: immunosuppressant
Dalfampridine : for walking
Cladrabine: doc for hairy cell leukemia, purine anti metabolite
Teriflunomide, inhibits DHOD
Leflunomide
Acting by Di hydro orotate dehydrogenase DHOD
Di methyl fumarate: immunosuppressant
Head to foot, use of anticholinergic
???
Valathamate
Used for cervical ripening
Atropine
Used for
Inocybe mushroom
OPC poisoning
Given in MG and cobra bite along with neostigmine
Along with diphenoxylate to reduce addiction
Sympathetic system
Tyrosine
Into dopa with the help of tyrosine hydroxylase
Dopa into dopamine with the help of dopa decarboxylase
Vesicular uptake of dopamine
Synthesis of NE can only take place in the vesicle from dopamine
with the help of hydroxylase
The vesicle acts as a storage for NE
Ca enters through the Ca channel
Vesicle reaches the nerve ending
Release of NE
Action alpha and receptor
NE can also be called as cathecholamine
Metabolized by COMT and MAO
But the termination of action is mainly by reuptake
Rate limiting step in synthesis of NE is tyrosine hydroxylase
In a case of pheochromocytoma, we can inhibit tyrosine hydroxylase
Drug is called Metyrosine( alpha methyl para thyrosine)
Phenoxybenzamine is the routine doc in pheochromocytoma
It is a non selective irreversible alpha blocker
blocker not given in pheochromocytoma coz of unopposed alpha
action
It should be given if the pt develops hypotension and reflex
tachycardia after phenoxybenzamine
During Sx
IV phentolamine or IV nitroprusside is given intra operative to
control HT
Atraumatic endoscopic Sx is the best
Halothane not given as it sensitizes the myocardium for arrythmia
Dopa decarboxylase enzyme blocker
Carbidopa
Benserazide
Role of carbidopa in parkinson
Dopamine controls behavior in pr frontal lobe
Over action here in the meso limbic pathway leads to psychosis
Nigro striatal pathway
Dopamine is responsible for initiation of movements in corpus
striatum
Ach is already there in striatum
Aging occurs
Neurons degenerate
Imbalance between Ach and dopamine
Hypokinesia, rigidity, tremor
Dopamine support corrects hypokinesia
Anticholinergics treat rigidity and tremor
Levodopa and carbidopa long term given
Chorea and athetosis
Psychosis
Tubero Infundibular
Hypothalamus to anterior pituitary
Dopamine controls prolactin secretion in pituitary
Prolactin release inhibiting factor: dopamine
If levodopa given alone
Levodopa gets transported by amino acid transport
So avoid giving with protein meal
Don't give with pyridoxine as it is a cofactor for dopa decarboxylase
Peripheral toxicity of levodopa
Nausea/ vomiting and altered taste sensation
Coz it stimulates CTZ
Levodopa induced vomiting should be treated by domperidone coz
metoclopramide crosses BBB and decreases levodopa efficacy
Dopamine can have
D1, 1, alpha 1
Too much of dopamine, affects Vaso motor center reducing outflow
cause hypotension
Levodopa is precursor of melanin, therefore absolutely CI in
malignant melanoma
Drug is IL-2 analogue: aldesleukin
Also given RCC
Levodopa can cause Mydriasis, thus CI in glaucoma
On (dyskinesia) and off ( severe Parkinsonism) phenomena
Off is more dangerous
Treated by
Rescue therapy
Subcutaneous apomorphine(D4)
Ondansetron not given with apomorphine as it causes hypotension
and loss of consciousness
Abrupt withdrawal
Neuroleptic malignant syndrome
Doc
Dantrolene
Acts on ryanodine receptor
Direct acting ms relaxant
Side effect is hepatotoxicity
Reserpine inhibits vesicular uptake of dopamine
Side effect is suicidal depression as there is no NE in the brain
Disulfiram inhibits hydroxylase, along with aldehyde dehydrogenase
Acetaldehyde causes headache, N/V,flushing, hypotension
Drugs causing disulfiram like reaction
C: chlorpropomide, cefoperazone
M: metronidazole
Praised: procarbazine
G: griseofulvin
T: tinidazole
Naidu: Nitrofurantoin
Adrenergic neuron blocker
Inhibit release of NE
Bretylium: class 3 anti arrythmic agent, chemical defibrillator, very
helpful in arrythmia due to bupivacaine( highly cardio toxic)
Therefore bupivacaine CI in IV regional anesthesia : Biers block
Controls ventricular arrythmia in hypothermia
Guanathidine
BP decreases
Postural hypotension
TCA and cocaine inhibit uptake of NE
Cocaine is a local anesthetic
Blocks Na channels
Causes HT
Metabolized by cyto P 450