Pharma Week 4 Flashcards
Mention 2 the major and minor mechanism for termination of Adrenergic action
The major mechanism of termination is
1_ neuronal re-uptake : termination of NEP action is mainly due to removal from the synabse back into the sympathetic nerve ending via NEP reuptake transporter system
2- vesicular uptake : for NEP that escape MAO degradation in mobile pool
The minor pathway
1- MAO in Brian and GIT
2- COMT in liver and brain and synapses
4 side effects of Adrenaline on CVS
1- tachycardia, palpitations
2- hypertension, worsen heart failure
3- Angina pectoris , Cardiac ischemia
4- Cerebral haemorrhage
One LABA and 2 SABA
1- salmeterol ( servent ) long acting in nocturnal asthma
1- Albuterol ( Salbutamol)
2- Terbutaline ( Bricanyl)
4 SE of B2 agonist
1- Tremor
2- Tolerance
3- Tachycardia
4- Bronchial hyperactivity
2 alpha 1 selective agonist and 4 usesc
Phenylephrine , Methoxamine
1- hypotension caused by spinal anesthesia
2- Nasal decongestant
3- Eye decongestant
4- Mydriasis in eye
2 Alpha 2 agonist and 4 side effect
Alpha methyl dopa :treat preeclampsia
Clonidine : treat nacrotic and alcohol withdrawal
1- dry mouth xerostomia
2- sedation
3- sexual dysfunction
4- hypertensive crisis if suddenly withdrawal
Indirect Acting symphathomimetics
Releasers
1- tyramine (red wine ,cheese )
2- amphetamine ( phsycostimulant -> due to DA , NE , 5HT release )
3- pseudoephedrine , ephedrine
Reuptake inhibitors
Cocacine , TCA , amphetamine
4 SE of amphetamine , ephedrine, cocaine
1- CNS : insomnia , anxiety,…
2- CVS : hypertension,…
3- Tolerance, dependence, addiction
4- Tachyphylaxis : after first dose due to depletion of biogenic amine
2 non selective alpha blocker, 1 use , 4 SE
1- phentolamine ( reversible)
2- phenoxybenzamine (irreversible)
1- pheochromocytoma
1- postural hypotension
2- Nasal congestion
3- Marked tachycardia
4- decrease libido
4 alpha 1 blocker and 3 therapeutic uses , 5 SE
Prazosin , terazosin , doxazosin : in HTN
Tamsulosin , alfuzosin : in BPH
Doxazosin : longest acting
1- hypertension
2- CHF ( decrease pre load , after load )
3- BPH : tamsulosin act on a1 A receptor
1- First does phenomenal : cause dizziness , vertigo and syncope to marked postural hypotension : about 30 minutes to 90 minutes after initial dose so prevented by using low doses at bedtime
2- reflex tachycardia
3- Nasal congestion
4- water retention so prevented by diuretics
5- decrease libido
Two selective alpha two receptor blocker
1- yohimbine
2- mirtazapine
Who doesn’t cause sedation in Beta blockers and 2 dosenot blood lipids
1- Atenolol
1- pindolol
2- Acebtulol
Why B blocker shouldn’t be given to diabetic patients
Masking hypoglycemic signs as hypoglycemia , tachycardia, anxiety and tremors which worn patient
7 SE of beta blockers
1- Bronchi constriction , CI in asthmatic
2- Rebound due to receptor up regulation
3- Bradycardia and heat block
4- sexual impairment
5- disturbance in metabolism : cause hypoglycemia and CI in diabetic patients as Masking hypoglycemic signs as tachycardia , anxiety, tremors which worn patient
6- Worsen acute heart failure by negative iontropic
7- CNS : sedation, sleep disturbances, depression fatigue ( lipid soluble as propranolol)
What to do in BBs overdose
Glucagon act on glucagon receptors and cause positive ionotropic and chronotropic due to Ga protein linked to adenyl cyclase
Details about Labetalol and carvedilol
Labetalol
It is used intravenous in hypertensive emergencies and orally in chronic hypertension.
Also is safe to be used in severe hypertension of pregnancy.
Carvedilol
It has an additional antioxidant property
Useful in chronic heart failure(anti-remodeling and improve mortality )
What is half life of Esmolol and use of it
Ultra Short actin BB
Rapidly metabolized by esterases of RBCs with t1/2 -> 10 minutes
Useful in arrhythmia associated with cardiac surgery
Therapeutic uses of BB in CVS , endocrinal , neurological, opthalmic , hepatic
Cardiovascular use
Mild to moderate hypertension, all beta blockers except esmolol
Chronic stable angina all except BBs with ISA
Subraventricular arrhythmia
Prophylactic after myocardial infarction : to decrease the incidence of sudden death
( propranolol, metoprolol , timolol)
Chronic heart failure : low dose of carvedilol , metoprolol, bisoprolol
Endocrinal uses
1-Hyper thyroidism : propranolol is used : is used to control tachycardia and inhibits the conversion of T4 to T3, which is the most active form
2- pheochromocytoma
Neurological uses
Tremor
Alcohol withdrawal manifestation
Acute panic symptoms
Prophylactic uses in migraine
Ophthalmic uses
Topical timolol reduce interocular pleasure and so used in open angle glucoma
Hepatic uses
Prevention of esophageal varicea bleeding in patients with portal hypertension caused by livers cirrhosis
