Le tadalafil possède une affinité marquée pour la PDE5, mais épargne en grande partie les isoformes PDE1, PDE2 et PDE11, réduisant ainsi le risque d’effets extra-caverneux. L’action se traduit par une augmentation contrôlée de la circulation sanguine locale, indépendante des variations alimentaires. Sa pharmacocinétique repose sur une absorption digestive rapide, un métabolisme hépatique par CYP3A4 et une distribution tissulaire large. La biodisponibilité reste stable, et l’équilibre plasmatique est atteint en quelques jours lors d’administrations répétées. Les interactions cliniquement significatives surviennent avec les inhibiteurs puissants de CYP3A4 tels que le kétoconazole. Dans la littérature pharmacologique, acheter cialis 20 mg est souvent associé à des schémas d’utilisation basés sur la durée prolongée de son action.

Microsoft powerpoint - cardiovascular pharmacology handout.ppt

Current Cardiovascular
Pharmacology
Arthur Jones, EdD, RRT
http://rc-edconsultant.com/
Learning Objectives:
Explain the actions, effects, indications,
adverse effects and precautions for
agents from the following drug
categories:
ƒcardiotonic agents
ƒantidysrhythmic agents
ƒnitrates
ƒmiscellaneous cardiovascular agents
Cardiotonic Agents
Epinephrine
Actions
alpha1- vasoconstriction
beta1
chronotropic- heart rate
inotropic- contractility
dromotropic- conductivity
beta2- smooth muscle relaxation
bronchodilation
vasodilation
Epinephrine
Effects:
increase systemic vascular resistance
(SVR) blood pressure (BP), peripheral
blood flow
increase coronary and cerebral blood
increase myocardial electrical activity
==> increased automaticity ==>
increased HR
increase myocardial contractility
increase myocardial 02 requirements
Epinephrine
Indications
ƒresuscitation
ƒshock, including anaphylaxis
ƒsevere asthma
Epinephrine
Routes
ƒIntravenous (IV)
ƒSubcutaneous (SC)
ƒEndotracheal tube (ETT)- double IV
Epinephrine
Adverse effects
ƒHypertension
ƒMyocardial infarction
ƒTachycardia
ƒPeripheral tissue blood flow
impairment (ischemia)
Norepinephrine (Levophed)
Actions- alpha, beta1 adrenergic
Effects
ƒincreased SVR ==> increased
ƒincreased HR
ƒpositive inotropic
Norepinephrine (Levophed)
Indication- neurogenic or septic
Adverse effects
ƒMyocardial hypoxia ==> infarction
ƒrenal failure
ƒHypertension
ƒNecrosis of exposed tissues
ƒPeripheral ischemia
Dopamine
Actions- alpha1, beta1 adrenergic,
dopaminergic
Effects (dose-dependent)
ƒLow dose- Cerebral, renal,
mesenteric vasodilation
ƒModerate doses- increase cardiac
ƒHigh dose- generalized
vasoconstriction
Dopamine
Indications:
ƒhypotension (shock)
ƒdecreased urinary output
Dopamine
Adverse effects
ƒTachycardia
ƒRenal necrosis
ƒPeripheral tissue necrosis
ƒdysrhythmias
Vasopressin (Pitressin)
Synthetic endogenous hormone-
antidiuretic hormone
Effects
ƒanti-diuresis
ƒvasocontriction
ƒstimulation of ACTH release
FYI - Click for more information on vasopressin
http://www.cvphysiology.com/Blood%20Pressure/BP016.htm
Vasopressin (Pitressin)
Indications
ƒcardiac arrest
ƒshock
septic
hypovolemic
ƒdiabetes insipidus- accompanies
head trauma
Neosynephrine (Phenylephrine)
Action- alpha adrenergic
Effect- potent vasoconstrictor
Indications:
ƒnon-hypovolemic shock
ƒmucosal edema- post-extubation??
ƒmucosal bleeding
ƒprolong action of local anesthetics
Adverse effects- tissue ischemia
Dobutamine
Actions- alpha, beta1, beta2 adrenergic
Effects:
ƒpositive inotropic ==> increased
cardiac output
ƒMild peripheral vasodilation ==>
decreased PVR, SVR, increased
coronary perfusion
ƒDoes NOT increase myocardial 02
ƒCombined with dopamine ==>
maintain BP, without increasing PAP
Dobutamine
Indications
ƒAcute congestive heart failure
ƒright ventricular failure
Milrinone (Primacor)
Action- phosphodiesterase inhibitor
Effects
ƒinotropic
ƒvasodilation
Milrinone (Primacor)
Indications
ƒcardiomyopathy
ƒcongestive heart failure
ƒpulmonary arterial hypertension
FYI - click for article on aerosolized milrinone for PAH
http://ejcts.ctsnetjournals.org/cgi/reprint/31/6/1081
Digitalis glycoside- digoxin
Action- increased Ca++ in
myocardium
Effects
ƒpositive inotropic
ƒnegative dromotropic ==>
depresses AV conduction
Digitalis glycoside- digoxin
Indication
ƒspecific dysrhythmias
ƒChronic CHF
Digitalis glycoside- digoxin
Adverse effects- digitoxicity more
likely with hypokalemia
ƒMultiple types of dysrhythmias
ƒAgitation
ƒNausea & vomiting
Antidysrhythmic Agents
Atropine
Action- parasympatholytic
Effects (cardiac)
ƒincreased SA node automaticity
==> increased HR
ƒincreased AV node conductivity
Atropine
Indications
ƒBradycardia
ƒHeart block
ƒAsystole- may be worth a try
Routes
ƒIV
ƒinstillation through ETT
Side effects- tachycardia
Lidocaine
Action- sodium channel blocker
Effects
ƒdecreased automaticity
ƒdecreased conductivity
ƒincreased threshold for
fibrillation
Indications- rapid ventricular
dysrhythmias
Lidocaine
Routes
ƒETT administration ==> double dose
ƒIV
Adverse effects
ƒPsychoses, seizures
ƒdecreased contractility
ƒHeart block- asystole
ƒincreased threshold for defibrillation
ƒLethal if given for heart block with
escape beats
Amiodarone (Cordarone)
Action- multiple ion channel
Effects
ƒdecreased AV conduction
ƒdecreased sinus node function
Indications- dysrhythmias
Adverse effects (circulatory:
ƒhypotension
ƒbradycardia
Amiodarone (Cordarone)
Adverse effects (pulmonary)-
occurs over days-years of treatment
ƒpulmonary oxygen toxicity
ƒinterstitial pneumonitis
ƒpulmonary infiltrates
ƒorganizing pneumonia ±
bronchiolitis obliteran (BOOP)
ƒpulmonary fibrosis
FYI - Link to download article on amiodarone toxicity
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC341704/pdf/thij00006-0073.pdf
Amiodarone (Cordarone)
Adverse effects (pulmonary):
ƒA-C membrane permeability
edema with or without ARDS
ƒalveolar hemorrhage
ƒbronchospasm
ƒlaryngeal edema
ƒanaphylactic shock
ƒpleural effusion
ƒpleural/pericardial thickening
Dronedarone (Multaq)
Indication - atrial fibrillation/flutter
Contraindications
ƒsevere heart failure
ƒliver disease
Less effective than amiodarone
Fewer adverse effects
Hepatotoxic
More expensive than amiodarone;
but, reduces hospitalization for AF
FYI - click to download article on dronedarone
http://www.nejm.org/doi/pdf/10.1056/NEJMoa0803778
Beta adrenergic blockers
Action- beta1 blockade
Effects
ƒdecreased HR
ƒdecreased vascular resistance
ƒdecreased contractility
ƒdecreased conductivity
ƒdecreased myocardial 02
consumption
Beta adrenergic blockers
Indications
ƒangina
ƒhypertension
ƒPost-MI
ƒInhibit ventricular response to
atrial flutter, fibrillation
Beta adrenergic blockers
Side effects
ƒHypotension
ƒCHF
ƒBronchospasm- non-selective
Beta adrenergic blockers
Agents
ƒpropanolol (non-selective)
ƒatenolol
ƒmetoprolol
ƒsotalol (Betapace)- non-selective
ƒesmolol- short duration of action
ƒnadolol (Corgard)- non-selective
ƒsotalol (Betapace)
Calcium Channel Blockers
action- block entry of Ca++ to
myocardium
indications
ƒangina
ƒdysrhythmias; e.g., PSVT
ƒhypertension
Calcium Channel Blockers
agents
ƒverapamil (Calan, Isoptan)
ƒdiltiazem (Cardizem)
ƒamlodipine (Norvasc)
Magnesium Sulfate
Action- replacement for depletion of
ƒmalnourishment
ƒalcoholism
Effects
ƒreverses torsades des pointes
ƒrelaxes bronchial smooth muscle
ƒrelaxes uterine muscle
Magnesium Sulfate
Indications:
ƒhypomagnesemia
ƒtorsades des points VT
ƒstatus asthmaticus
ƒpre-eclampsia/eclampsia
Adverse effects- minimal
Nitrates
Sodium nitroprusside (Nipride)
Effects- vasodilation, arterial and
Indications
ƒHypertensive emergency
ƒLV failure
Sodium nitroprusside (Nipride)
Adverse effects
ƒcyanide poisoning
ƒhypotension
Precaution- avoid exposure of agent to
Nitroglycerine
Effect- decreased SVR ==> decreased
afterload and preload
Side effects- hypotension, headache
Indication- angina pectoris, AMI
Preparations- sublingual tablets, IV,
Miscellaneous Agents
Nesiritide (Natrecor)
Synthetic recombinant brain natriuretic
peptide (BNP)
ƒpotent vasodilator
ƒrapid reduction in PCWP
FDA approval in 2001
Indication
ƒsevere decompensated CHF
ƒdyspnea at rest or minimal activity
FYI - click for article on nesiritide
http://ccn.aacnjournals.org/content/26/1/39.full.pdf
Nesiritide (Natrecor)
Contraindications
ƒlow filling pressures
ƒhypotension
Adverse effects
ƒkidney failure
ƒdeath
ƒlitigation
Angiotensin converting enzyme (ACE)
inhibitors
action- block conversion of
angiotensin I to angiotensin II
effect- vasodilation
indications
ƒhypertension
ƒheart failure
side effect- chronic, dry cough
Angiotensin converting enzyme (ACE)
inhibitors
side effects
ƒchronic, dry cough
ƒangioedema- airway obstruction
FYI - click for more information on ACE inhibitors
http://www.chfpatients.com/ace.htm
ACE inhibitors
agents
ƒlisinopril (Zestril), (Prinivil)
ƒramipril (Altace )
ƒenalapril (Vasotec )
ƒbenazepril (Lotensin)
ƒcaptopril (Capoten)
Summary & Review
Cardiotonic agents- simulatory
cardiovascular effects
ƒepinephrine
ƒnorepinephrine
ƒdopamine
ƒdobutamine
ƒmilrinone
ƒvasopressin
ƒdigitalis
Summary & Review
Antidysrythmic agents
ƒAtropine
ƒLidocaine
ƒAmiodarone
ƒBeta adrenergic blockers
ƒCalcium channel blockers
ƒMagnesium sulfate
Summary & Review
Nitrates- vasodilators
ƒsodium nitroprusside
ƒnitroglycerine
Miscellaneous agents
ƒnesiritide- vasodilator for severe CHF
ƒACE inhibitors- antihypertensive

Source: http://www.respiratorycare-online.com/lecture_series/cardio_pharm_mp3/cardio_pharm_handout.pdf