Surfactant Agents

 

I.                  Definitions

a.    Surfactant:  A surface-active agent that lowers surface tension

                                                 i.      Examples

1.    soap

2.    detergent

b.    Surface Tension:  Force caused by attraction between like molecules that occurs at liquid-gas interfaces and that holds the liquid surface intact

                                                 i.      Units of Measure: dynes/centimeter (dyn/cm)

1.    the force required to cause a 1 cm rupture in the surface film

                                               ii.      a droplet forms because a liquid’s molecules are more attracted to each other than the surrounding gas

c.     LaPlace’s Law:  Physical principle that describes and quantifies the relationship between the internal pressure, amount of surface tension and the radius of a drop or bubble

                                                 i.      In the alveoli where there is a single air-liquid interface, LaPlace’s Law is: Pressure=(2 x ST)/ r, where

1.    ST = surface tension

2.    r = radius of the alveoli

 

II.              Application to the Lung

a.    Increased surface tension can cause collapse or difficulty opening the alveoli

                                                 i.      Surfactant lowers the surface tension to decrease the pressure needed to open the alveoli

b.    In pulmonary edema, the surface tension of the liquid allows the formation of a bubbly froth

                                                 i.      Lowering the surface tension will cause the foam bubbles to collapse and liquefy

 

III.           Clinical Indications for Exogenous Surfactants

a.    Prophylactic Treatment

                                                 i.      Prevention of RDS in very-low-birth-weight infants and infants with higher birth weights who have evidence of immature lungs, at risk for developing RDS

b.    Rescue Treatment

                                                 i.      Retroactive or “rescue” treatment of infants who have developed RDS

1.    the basic problem in RDS is lack of pulmonary surfactant as a result of lung immaturity

2.    increased ventilating pressure is required to expand the alveoli during inspiration, which will lead to respiratory failure

 

IV.            Previous Surfactant Agents in Respiratory Care

a.    Ethyl alcohol

                                                 i.      Application

1.    used for treating pulmonary edema

2.    was given by nebulizer

a.    3 - 5 ml. of 30 - 50% solution

                                               ii.      Mode of Action

1.    alcohol lowered the surface tension of the foamy exudate, reducing it to a liquid, clearable state

                                             iii.      Disadvantages

1.    efficacy not proven

2.    toxic to membranes

3.    better alternatives are available today

b.    Mucus Wetting Agents (Detergents)

                                                 i.      Examples

1.    Alevaire

2.    Tergamist

                                               ii.      Indication

1.    to improve water penetration and facilitate transport and expulsion of adhesive mucus

                                             iii.      Mode of Action

1.     these agents may interact with mucus to produce emulsification

a.    The mucus will dissolve or disperse into smaller molecules

                                            iv.      Efficacy

1.    efficacy in vivo is not proven

c.     Phospholipids

                                                 i.      Coating of the airway epithelium by phospholipids may serve as a lubricant for mucus transport

                                               ii.      May offer another alternative to normalizing mucociliary transport and mucus clearing in disease states causing mucus hypersecretion or decreased clearance of secretions

                                             iii.      There are no agents in general clinical use at this time

 

V.                Exogenous Surfactants

a.    Exogenous

                                                 i.      Originating outside the body

1.    other humans

2.    animals

3.    laboratory synthesis

b.    Clinical Use

                                                 i.      to replace missing or immature surfactant in premature infants

                                               ii.      investigated for use in adults with disease processes that have low surfactant (ARDS)

c.     History and Development of Exogenous Surfactants

 

Year

Event

1929

Von Meergaard showed that lungs were more difficult to inflate with air than with fluid

1956

Clements measured the surface tension of lung fluid extracts

1958

Dipalmitoylphosphatidylcholine (DPPC) is identified by Clements and associates as the main surface-active component of pulmonary surfactant

1959

Avery and Mead showed that surface tension is higher in the lungs of infants with hyaline membrane disease than in the lungs of normal infants

1964

Aerosols of synthetic DPPC are attempted in RDS, with little success

1972

Enhorning and Robertson demonstrate the effectiveness of surfactant replacement in premature animals

1980

Fujiwara and associates report success in exogenous surfactant therapy in infants, using “lyophilized artificial surfactant” (bovine extract, Surfactant TA)

1990

Colfosceril palmitate (Exosurf Neonatal, Burroughs Wellcome) approved for general use

1991

Beractant (Survanta, Ross Laboratories) approved for general use

1998

Calfactant (Infasurf, Forest Pharmaceuticals) approved for general use

1999

Poractant alfa (Curosurf, Dey Labs) approved for general use

 

VI.            Composition of Surfactant

a.    Lipids (85-90%)

                                                 i.      Phospholipids (~90%)

1.    Phosphatidylcholine

a.    Dipalmitoylphosphatidylcholine (DPPC)

                                                                                                                         i.      most prominent in reducing surface tension

2.    phosphotidylglycerol

3.    phosphatidylethanolamine

4.    phosphatidylserine

5.    phosphatidylinositol

6.    spingomyelin

                                               ii.      Neutral Lipids (10%)

1.    cholesterol and others

b.    Proteins (10%)

                                                 i.      Surfactant protein A (SP-A)

1.    regulates secretion and reuptake of surfactant to Type II cell

                                               ii.      Surfactant protein B (SP-B)

1.    improves spreading of phospholipids in the alveolus

                                             iii.      Surfactant protein C (SP-C)

1.    improves spreading of phospholipids in the alveolus

                                            iv.      Surfactant protein D (SP-D)

1.    no clear role

 

VII.         Production and Regulation of Surfactant

a.    Production

                                                 i.      Synthesized in the type II alveolar cells

                                               ii.      Stored in vesicles called lamellar bodies

                                             iii.      Secreted by exocytosis into the alveolus

                                            iv.      The major stimulus for secretion is inflation of the lung

b.    Regulation

                                                 i.      Endocytosis back into the type II cell

1.    most surfactant (90-95%) is taken back into the type II cell, reprocessed, and resecreted

a.    this is the reason that exogenously administered surfactant is successful in replacing missing surfactant with one or two doses

                                               ii.      Clearance/degradation by alveolar macrophages

 

VIII.     Others Benefits of Surfactant

a.    Contributes to host defense

                                                 i.      Increased bacterial killing

                                               ii.      Modifies macrophage function

                                             iii.      Down-regulates the inflammatory response

1.    decreases mediator release

                                            iv.      enhances ciliary beat frequency

 

IX.            Types of Exogenous Surfactant Preparations

 

Category

Description

Examples

Natural

Surfactant from natural sources (human or animal) with addition or removal of substances)

Survanta (bovine)

Surfactant TA (bovine

Curosurf (porcine)

Infasurf (bovine)

Alveofact (bovine)

Synthetic

Surfactant that is prepared by mixing in vitro synthesized substances that may or may not be in natural surfactant

Exosurf

ALEC

Synthetic natural

Surfactant prepared in vitro with genetic engineering

None at present

 

 

X.                Specific Exogenous Surfactant Preparations

a.    Colfosceril palmitate (Exosurf Neonatal)

                                                 i.      Indications

1.    Prophylactic  therapy of infants weighing less than 1350g birth weight

2.    Prophylactic therapy of infants with birth weights greater than 1350g with evidence of pulmonary immaturity and at risk for RDS

3.    Rescue treatment of infants who have developed RDS

                                               ii.      Dosage

1.    5 ml/kg of the reconstituted suspension q12° X 2 - 3 doses

                                             iii.      Preparation

1.    available as a dry powder that is reconstituted with 8 ml sterile water prior to use

                                            iv.      Administration

1.    instilled directly into the endotracheal tube through a side port adapter attached to ET tube, in 2 divided aliquots

a.    1st half of dose in midline position

                                                                                                                         i.      infant rotated to the right and ventilated for 30 seconds

b.    2nd half of dose in midline position

                                                                                                                         i.      Infant rotated to the left and ventilated for 30 seconds

2.    a single vial can treat up to a 1600 g infant

a.    5 ml/kg x 1.6 kg = 8 ml                  

 

b.    Beractant (Survanta)

                                                 i.      Indications

1.    Prophylactic therapy of premature infants less than 1250g birth weight or with evidence of surfactant deficiency and risk of RDS

2.    Rescue treatment of infants with evidence of RDS

                                               ii.      Dosage

1.    4 ml/kg (100 mg/kg) of the suspension q6°

                                             iii.      Preparation

1.    available as a vial containing 8 ml of suspension with 200 mg active ingredient (25 mg/ml)

                                            iv.      Administration

1.    instilled directly into the endotracheal tube through a 5-French catheter, in 4 divided aliquots

2.    the infant is placed in 4 different positions and manually or mechanically ventilated for 30 seconds

3.    a single vial can treat up to a 2000 g infant

a.    4 ml/kg x 2 kg = 8 ml

                                              v.      Handling

1.    keep refrigerated

2.    warm at room air for at least 20 minutes prior to administration

3.    unopened vial may be returned for refrigeration within 8 hours

4.    used vials should be discarded

 

c.     Calfactant (Infasurf)

                                                 i.      Indications

1.    The prevention of RDS in premature infants < 29 weeks of gestational age at high risk for RDS

2.    Rescue treatment of premature infants less than or equal to 72 hours of  age who develop RDS and require endotracheal intubation

                                               ii.      Dosage

1.    3 mL/kg  of the suspension q12 h up to 3 doses

                                             iii.      Preparation

1.    available as a vial containing 6 ml of suspension with 210 mg of active ingredient

                                            iv.      Administration

1.    Side-port adapter

a.    The dose in given in two aliquots

                                                                                                                         i.      Position the infant with either the right or left side dependent

                                                                                                                       ii.      Administer half the dose in small bursts to coincide with the inspiratory cycle, over 20 to 30 breaths

                                                                                                                     iii.      Reposition and administer the other half of the dose in the opposite position

2.    Catheter

a.    The dose is given in four aliquots, with the catheter removed between each instillation

b.    Each portion is given with the infant in a different position

                                                                                                                         i.      Prone

                                                                                                                       ii.      Supine

                                                                                                                     iii.      Right lateral

                                                                                                                    iv.      Left lateral

c.     The infant is ventilated for 0.5 to 2 minutes between portions

3.    a single vial can treat up to a 2000 g infant

a.    3 ml/kg x 2 kg = 6 ml

 

d.     Poractant alfa (Curosurf)

                                                 i.      Indications

1.    For the treatment or rescue of RDS in premature infants

2.    Unlabeled Uses

a.    Prophylaxis for RDS

b.    ARDS resulting from viral pneumonia

c.     HIV-infected  infants with Pneumocystis carinii pneumonia (PCP)

d.    ARDS after near-drowning

                                               ii.      Dosage

1.    2.5 mL/kg

2.    Repeat doses of 1.25 mL/kg birth weight q12h x 2

                                             iii.      Preparation

1.    two preparations available

a.    a vial containing 1.5 ml of suspension containing 120 mg of active ingredient

b.    a vial containing 3.0 ml of suspension containing 240 mg of active ingredient

                                            iv.      Administration

1.    instilled directly into the endotracheal tube through a 5-French catheter

a.    The dose is given in two aliquots

                                                                                                                         i.      Each portion is given with the infant in a different position

1.    right side dependent

2.    left side dependent

                                                                                                                       ii.      The catheter is removed between portions and the infant is manually ventilated with 100% O2 for 1 minute

2.    a single 3.0 ml vial can treat up to a 1200 g infant

a.    2.5 ml/kg x 1.2 kg = 3 ml

 

XI.            Mode of Action

a.    Exogenous surfactants replace and replenish a deficient endogenous surfactant pool in neonatal RDS

                                                 i.      Increased FRC

1.    dramatic improvement in oxygenation

 

XII.         Hazards and Complications of Surfactant Therapy

a.    During instillation

                                                 i.      airway occlusion

1.    relatively large volumes are instilled into the ETT

                                               ii.      desaturation

1.    impaired diffusion

                                             iii.      bradycardia

1.    heart rate < 100 bpm in a neonate

a.    normally 120-160 bpm

2.    caused by hypoxia and vagal stimulation

b.    Post-instillation

                                                 i.      high arterial oxygen (PaO2) values

1.    wean O2 to maintain PaO2 50-70 torr

                                               ii.      over-ventilation and hypocarbia

1.    decrease ventilating pressures as compliance improves to prevent barotraumas

                                             iii.      apnea

1.    irritation to the airway causes apnea in a neonate

                                            iv.      pulmonary hemorrhage

1.    factors that increase risk

a.    < 700 g birth weight

b.    younger

c.     male

d.    patent ductus arteriosus (PDA)

 

XIII.     Factors in Surfactant Selection

 

Parameter

Synthetic (Colfosceril)

Natural (Beractant)

Response time

Slower in onset (several hours)

Rapid in onset (5-30 min)

Administration

During mechanic ventilator breath

Removed from ventilator

Drug preparation

Must reconstitute before use

Refrigerated suspension; must warm prior to use

Side effects

No proteins to stimulate immune response; no infectious agents present

Proteins may elicit immune response; concern over sterilization effectiveness

Cost

Similar

Similar

 

 

XIV.       Benefits of Surfactant Therapy

a.    Improved survival in RDS

b.    Increased oxygenation

c.     Decreased days of ventilatory support and supplemental O2